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NOVEL DRUG
DELIVERY SYSTEM
GROUP NO. 06
Novel Drug delivery System (NDDS) refers to
the approaches, formulations, technologies,
and systems for transporting a pharmaceutical
compound in the body as needed to safely
achieve its desired therapeutic effects.
•Advantages of Novel Drug Delivery System are:
1.Optimum dose at the right time and right location.
2.Efficient use of expensive drugs, excipients and reduction in production cost.
3.Beneficial to patients, better therapy, improved comfort and standard of living.
ASRA HAMEED
12859
ORAL ROUTE OF
Introduction
Despite tremendous innovations in drug
delivery, the oral route remains the
preferred route for administration of
therapeutic agents because of accurate
dosage, low cost therapy, self medication,
noninvasive method, and ease of
administration leading to high level of
patient compliance.
Rapidly
Dissolving
Tablets (RDTs)
Formulation of RDT’s
• Molded tablets are prepared by forcing
dampened powders under low pressure
into die cavities.
• Solidification depends upon crystal
bridges built up during the subsequent
drying process.
• Molded tablets made from completely
and readily water-soluble ingredients
• They are employed orally, or where rapid
drug availability is required such as in
the case of Nitroglycerin Tablets,
sublingually.
Preparation of Molded Tablets
• Molded tablets are prepared from mixtures of medicinal
substances and a diluent usually consisting of lactose and
powdered sucrose in varying proportions.
• The powders are dampened with solutions containing high
percentages of alcohol.
• The dampened powders are pressed into molds, removed, and
allowed to dry.
• Molded tablets are quite friable and care must be taken in
packaging and dispensing.
Lyophilization
• The drug is dissolved or dispersed in an aqueous
solution of a carrier.
• The mixture is poured into the wells of the preformed
blister packs.
• The trays holding the blister packs are passed through
liquid nitrogen freezing tunnel to freeze the drug
solution.
• Then the frozen blister packs are placed in refrigerated
cabinets to continue the freeze drying.
• Finally the blisters are packaged and shipped.
• Characteristics: The preparations are highly porous,
have high specific surface area, dissolve rapidly and
ultimately show improved absorption and bioavailability.
STEPS INVOLVED IN LYOPHILIZATION
FREEZING STAGE
SECONDARY DRYING STAGE**
* The temperature and pressure should be below the triple point of water i.e.,
0.0098°C and 4.58mmHg. Easily removes moisture up to 98% to 99%.
** The temperature is raised to 50°C – 60°C and vacuum is lowered about
50mmHg. It takes about 10-20 hrs.
Lyophilization
• Advantage
Water sensitive drug are
prepared by this
method as RDTs
instead of dry-
granulation (delay DT)
• Disadvantage
Some portion of drug
remains in the wells of
the blister packs
EXAMPLES
Loratidine (Claritin Reditab and Dimetapp Quick Dissolve)
Cisapride monohydrate (Propulsid Quicksolv)
Risperidone (Risperdal M-tab)
Ibuprofen (Nurofen Flashtab)
Direct Compression
• A direct compression method uses conventional
equipment, commonly available excipients, and a limited
number of process steps.
• The direct compression tablet's disintegration and
solubilization are based on the single or combined
action of super disintegrants, water-soluble
excipients, and effervescent agents.
• The choice of superdisintegrant for a tablet formulation
depends largely on the nature of the drug being used.
• TizanidineHCl,OxybutyninHCl,Rofecoxib,and Ethenzamide
are some examples of model drugs that have been formulated
as RDT by direct compression method.
Super
Disintegrants
Used In Rapid Disintegrating Tablets
Croscarmellose Sodium
 Synonyms: (Ac-Di-Sol)
 Cross linking makes it an insoluble, hydrophilic,
highly absorbent material, resulting in excellent
swelling properties and its unique fibrous nature
gives it excellent water wicking capabilities.
 Croscarmellose sodium provides superior drug
dissolution and disintegration characteristics, thus
improving bioavailability of formulations
CROSPOVIDONE
 Synonyms:- Crosslinked polyvinylpyrrolidone
(PVP), Insoluble PVP, Polyvinylpolypyrrolidone
(PVPP), Crospovidone , Crospovidonum
 Crospovidone, NF, is a synthetic, insoluble but
rapidly swellable, cross-linked homopolymer of
N-vinyl-2-pyrrolidone
Sodium Starch Glycolate
 Synonyms: Carboxymethyl starch, Explotab,
Primojel
 Primojel promotes water penetration into the
tablet and develops a disintegration force
needed to push the particles apart.
 High swelling capacity results in its high
disintegration rate and efficiency.
PHARMACEUTICAL LOLLIPOPS
Pharmaceutical
Lollipops
• Lollipops have been used to deliver pharmaceuticals
(chiefly, Lipophilic drugs) to patients.
• Provide rapid absorption into the blood stream through the
mucosa of the mouth
• Absorption occurs much more rapidly than when drugs are
swallowed and absorbed via the digestive system.
• The dose can easily be controlled by administering the
lollipop only until the desired effect is observed, thereby
minimizing the dose
• Lollipops provide a pleasant way for a reluctant patient to
receive the pharmaceutical.
Pharmaceutical
Lollipops
• In particular, lollipops containing the potent,
short-acting narcotic fentanyl have been
approved by the FDA for the treatment of severe
pain.
• For example: Actiq by Cephalon
Fentanyl Lollipop
• It is a solid formulation of fentanyl citrate on a plastic stick
that dissolves slowly in the mouth for absorption across the
buccal mucosa.
• It is effective in treating cancer breakthrough pain and other
problems, such as bone injuries, migraines, severe back
pain, cluster headaches, neuropathy, arthritis, and moderate
to severe chronic, non-malignant pain.
• The dosage unit is a white, berry-flavored lozenge on a stick
which is swabbed on the buccal mucosa, between cheek and
gum to release the fentanyl quickly into the bloodstream.
Fentanyl Lollipop
Absorption
•Normally 25% of the drug is absorbed via the buccal
mucosa directly into the bloodstream while the remaining
75% is swallowed and then slowly absorbed in the
gastrointestinal tract.
•Two-thirds of the swallowed dose is metabolized by the
liver and becomes unavailable
•25% of the total dose will reach the bloodstream via the
intestines
•50% of the total dose will reach the bloodstream via both
routes
Fentanyl Lollipop
Side effects
•Sedation
•Nausea
•Constipation
•tolerance
•respiratory depression
•dental decay
•Each lozenge contains approx. 2grams of sugar, and
has issues for pre-diabetic users and diabetic users.
References
• Fast disintegrating tablets: Opportunity in drug delivery system, Ved
Parkash, Saurabh Maan, Deepika,Shiv Kumar Yadav, Hemlata, and
Vikas Jogpal, J Adv Pharm Technol Res. 2011 Oct-Dec; 2(4): 223–
235. doi: 10.4103/2231-4040.90877
• Md.Nehal Siddiqui*, Garima Garg, Pramod Kumar Sharma, FAST
DISSOLVING TABLETS: PREPARATION, CHARACTERIZATION
AND EVALUATION: AN OVERVIEW, Volume 4, Issue 2,
September – October 2010; Article 015,page 87-96 ISSN 0976 –
044X
• System for delivering pharmaceuticals to the buccal mucosa , US
6103257 A, http://www.google.com/patents/US6103257
• https://en.wikipedia.org/wiki/Actiq
AISHA ABDULLAH
12850
TOPICAL ROUTE OF ADMINISTRATION
TRANSDERMAL ROUTE
• Transdermal patch is a medicated
adhesive patch that is placed on skin to
deliver a spacific dose of medication
through skin & into the blood stream.
• Attractive alternative to the conventional
drug delivery methods of oral
administration & injection.
LATEST APPROACHES
• Various technologies have been
developed to by pass or modulate barrier
function of skin.
1-IONTOPHORESIS
• Effective & painless method of delivering
medication to a localized tissue area by
applying electrical current to a solution of
the medication.
2-ELECTROPORATION
• Intense electric charges create small pores in
phospholipid bilayer of cell membranes can
assist in transdermal delivery of drugs.
• Appears to reversibly disrupt the lipid bilayers
in stratum corneums & channels it creates are
said to promote the passage
of hydrophilic drugs through
skin.
3-PHONOPHORESIS
• Use of ultra sound of a suitable frequency to
enhance skin permeability seems to be a
useful alternative method for delivering drugs
through skin & can be applied to vaccination &
gene therapy.
• Also known as sonophoresis.
4-MICRONEEDLES
• Patches coated with hundreds of microscopic
needles can deliver proteins, Nano particles &
both small & large molecules through skin.
NEELAM SHARIF
12886
OPTHALMIC ROUTE OF ADMINISTRATION
Ophthalmic
Preparations
• Ophthalmic preparations are the specialized dosage forms
designed to be instilled on to the external surface of the eye
(topical) administered inside (intraocular) or adjacent
(periocular) to the eye.
• The most commonly employed ophthalmic dosages are:
 Solutions
 Suspensions
 Ointments
• The newest dosage forms for ophthalmic delivery are:
 Gel-Forming Solutions(Situ Gels)
 Ocular Inserts
 Contact lenses with drugs
Ophthalmic
Preparations
•Ophthalmic preparations are
sterile products that are intended
to be applied to the eyelids or
placed in the space between the
eyelids and the eyeball .
•One of the problems associated
with the use of ophthalmic
solutions is the rapid loss of
administered drug due to the
blinking of the eye and the flushing
effect of lacrimal fluids lost through
tears.
Ophthalmic Novel
Drug Delivery
System
Ocular Inserts
Inserts are solid or semisolid dosage forms without disadvantages of
traditional ophthalmic drug forms . show the ability to stay in conjunctival sac
for a longer period, and are more stable than conventional dosage forms.
Polymeric materials most often employed in developing inserts include, for
example, methylcellulose and its derivatives, that is, hydroxypropyl
methylcellulose (HPMC) etc
Advantages:
Accurate dosing
The possibility of slow substance release with constant speed
Limiting its systemic absorption. Moreover, using them enables reduction of
the drug application frequency,
Decrease adverse effects and blurring of vision occurrence.
Ocusert device
• Example of this is the Ocusert Device for pilocarpine membrane-controlled
delivery.
• Pilocarpine is available in a membrane controlled reservoir system that is used in
the treatment of glaucoma.
• Pilocarpine is sandwiched between two EVA membranes. It also contains alginic
acid, a seaweed carbohydrate, which serves as a carrier for Pilocarpine .
• The small, clear device has a white annular border made of EVA copolymer
impregnated with titanium dioxide (pigment) that makes it easier for the patient to
see.
• The insert is placed in the cul-de-sac, where it will float with the tears. The
Pilocarpine will diffuse from the device and exert its pharmacologic effect
Ophthalmic Inserts
Lacrisert
This medications is an insert that is placed in your eye
to treat dry eye. It is usually used when an artificial
tears solution is not successful. It is used to treat
certain other eye disorders ( keratitis , decreased
corneal sensitivity)
Lacrisert is a rod-shaped watersoluble form of
hydroxypropyl cellulose. The insert is placed in the
inferior cul-de-sac of the eye once or twice daily for
the treatment of dry eyes. The inserts soften and
slowly dissolve it help in thickening the precorneal tear
film and prolonging the tear film breakup.
Gel-forming solutions
They are semisolid viscous liquids,
showing the ability to undergo sol-
to-gel transitions when influenced
by external factors, like
appropriate pH, temperature, and
the presence of electrolytes. This
property causes slowing of drug
drainage from the eyeball surface
and increase of the active
ingredient bioavailability. Polymers
employed in developing these
drug.
Gel Extended Release
Product
• Certain preparations are designed to prolong the action of drug or
to extend the action of drug
• One example of these Ophthalmic Product in which viscosity
increasing agents are used to increase the corneal contact time of
drug i.e.
• Timolol maleate ( Timoptic -XE, Merck) employs gellan gum which
forms a gel upon contact with the precorneal tear film.
Contact Lenses Coated
with Drugs
• . This drug form can absorb on its surface water-
soluble substances, released after applying the
drug over the eyeball for a longer period of time.
The first and most widely used polymer in the
production of lenses was the cross-linked poly
(2-hydroxyethyl methacrylate) with small amount
of ethylene glycol dimethylacrylate.
• In recent years, research has been conducted on
employing silicon-based lenses. Interest in contact
lenses still grows.
• Examples of drugs whose pharmaceutical
availability from lenses was researched include
timolol , ciprofloxacin , dexamethasone , and
cyclosporine .
SABIHA GUL
131027
Implants
Definition
• Implants are small sterile solid masses consisting of a
highly purified drug (with or without occupants) made by
compression or molding or extrusion.
• Implants are drug delivery systems which provide
controlled delivery of drug over a period of time at the
site of implantation
Introduction
• Implants are intended for implantation in the body
(usually subcutaneously) for the purpose of providing
continuous release of the drug over long periods of time.
• Implants are administered by means of a suitable special
injector or surgical incision.
• These are developed with a view to transmit drugs and
fluids into the blood stream without the repeated
insertion of needles
• These systems are particularly suited for delivery
requirements of drugs such as insulin, steroids,
antibiotics, analgesics, heparin, total parenteral nutrition
etc.
Types of implants
Advantages
Unattended continuous delivery within the therapeutic window
Avoids the highly variable peak and trough concentrations
Enhanced drug efficacy
Minimized side effects
Termination of therapy as and when required
Patient compliance is also a benefit of continuous dosing with
these implants as they operate for a long period of time once
implanted
Disadvantages
The reaction between host and implant.
Implantation procedure is difficult in the case of larger
implants.
Inadequate release.
Requires small surgery for large implantation & painful.
Application
A. Cancer Treatment
Gliadel Wafer: Delivers carmustine for the treatment of brain tumours
directly at the site of tumour to prevent reccurrence of tumours.
Depocyte: cytarabine releasing implantable DDS used to treat acute
leukemia.
Duros osmotic pump: Non-biodegradable implantable DDS used to
deliver Leoprolide acetate in the treatment of prostate cancer.
B. Osteoporosis
Micro chips: This device made by ELI Lilly & coworkers used to
deliver Forteo drug used to increase bone density in patients suffering
from severe osteoporosis.
D. Contraceptives
Norplant: delivers Norgestrol to achive contraception.
Reactions of host to implant:
Changes in permeability of polymer to body fluids.
Environmental stress cracking.
Chemical breakdown of polymeric material.
Loss of tensile strength in case of hydrophobic polymers.
C. Ocular Diseases
Lacrimedics: these are collagen implants used to treat dry eye syndrome
by partially blocking tear removing canals and they dissolve within 7-10
days.
Vitrasert: delivers ganicyclovir used to treat AIDS related retinitis.
NOSHEEN HAYAT
131018
VAGINAL ROUTE OF
Novel concept in vaginal
drug delivery
• NVDDS are designed with desirable
distribution, bio adhesive, retention and
release characteristic.
ADVANTAGES
• Ease of administration
• Reduce side effects
• Avoids first pass metabolism
• Effective for orally inactive drugs
• High vascularization
• Low enzymatic activity.
DISADVANTAGES
• Local irritation of some drugs
• Personal hygiene
• Gender specificity
• Influence of sexual intercourse
• Cultural sensitivity
• Some of drugs are sensitive to vaginal pH. 37
RECENT ADVANCES IN
VAGINAL DRUG DELIEVRY
Achieved by the use of
• bio adhesive and
• other novel delivery system
Bio adhesives delivery
systems
Bio adhesive vaginal formulations that are
capable of delivering the active agent for
an extended period at a predictable rate
Other novel delivery
systems
• Phase change polymers
• Formulations based on a thermoplastic
graft co polymer
Evaluation Of Vaginal
Formulations
• In Vitro studies
• In vivo studies
Recent developments
• Effervescent vaginal tablets of nystatin
• Bio adhesive effervescent ketoconazole
tablets
APPLICATIONS OF INTRA VAGINAL
DRUG DELIEVERY SYSTEM
• Vaginal immunization
• Treatment of HIV infection
• Treatment of local fungal infection
• Delievery of hormones
• Multi-cycle administration of vaginal
contraceptive rings
Vaginal ring
Vaginal rings are 'doughnut-shaped' polymeric drug delivery
devices designed to provide controlled release of drugs to
the vagina over extended periods of time.
Several vaginal ring products are currently available, including:
Femring :
a low-dose estradiol-acetate releasing ring, manufactured from
silicone elastomer, for the relief of hot flashes and vaginal
atrophy associated with menopause.
NuvaRing:
a low-dose contraceptive vaginal ring, releasing progesterone
and estrogen.
60
ZABAB KHAN
131066
URETHRAL ROUTE OF ADMINISTRATION
URETHRAL ROUTE OF
ADMINISTRATION
• The urethral route of administration is application of drug
by insertion into the urethra
• Common dose forms include:
◦ solutions
◦ suppositories
• Urethral delivery may be used to treat
◦ incontinence
◦ impotence in men
• Disadvantages
◦ inconvenience
◦ localized pain
ALPROSTRADIL
URETHRAL MICROSUPPOSITORY
• Single used
• 1.4 mm in diameter and 3-6mm in
length
• Strengths available: 125,150,250,500 and
1000 microgram/units
• Inserted with the help of device
• Suspended in PEG
• Self insert and removal
• Sustain delivery for 4-7days
Research
Articles
NOVEL DRUG DELIVERY SYSTEM
PHARMACEUTICS & NOVEL
DRUG DELIVERY SYSTEMS
Tariq Jamshaid
Surge Laboratories Private Limited, Pakistan
Novel Drug delivery System (NDDS) refers to the approaches, formulations,
technologies, and systems for transporting a pharmaceutical compound in the body
as needed to safely achieve its desired therapeutic effects. It may involve scientific
site-targeting within the body, or it might involve facilitating systemic
pharmacokinetics; in any case, it is typically concerned with both quantity and
duration of drug presence. Novel Drug delivery is often approached via a drug's
chemical formulation, but it may also involve medical devices or drug-device
combination products. Drug delivery is a concept heavily integrated with dosage form
and route of administration. NDDS is advanced drug delivery system which improves
drug potency, control drug release to give a sustained therapeutic effect, provide
greater safety, finally it is to target a drug specifically to a desired tissue. NDDS is a
system for delivery of drug other than conventional drug delivery system. NDDS is a
combination of advance technique and new dosage forms which are far better than
conventional dosage forms.
Advantages of Novel Drug Delivery System are: 1. Optimum dose at the right time
and right location. 2. Efficient use of expensive drugs, excipients and reduction in
production cost. 3. Beneficial to patients, better therapy, improved comfort and
standard of living.
Basic modes of novel drug delivery systems are: 1. Targeted Drug Delivery System 2.
Controlled Drug Delivery System 3. Modulated Drug Delivery System
Factors affecting the design of controlled release products are: 1. Physicochemical
properties of a drug 2. Route of administration 3. Acute/Chronic therapy 4. Target
sites 5. The Patient 6. The disease state/leve.
CURRENT TRENDS IN NOVEL
OPHTHALMIC DRUG DELIVERY
SYSTEM: AN OVERVIEW
Sidra Farooq, Mirza Yasir Hussain and Syed Muhammad Farid
Hassan
Department of Pharmaceutics, Faculty of Pharmacy, University of
Karachi, Main University Road, Karachi
One of the most daring tasks faced by the
pharmaceutical researchers is the ophthalmic drug
delivery. Their aim is to achieve and sustain a
therapeutic level at the site of action for extended
period of time. Therefore, to withstand drug levels at
the target site for a sufficient time, novel drug delivery
techniques are developed. Ophthalmic drug delivery
route has seen significant advancement for future
perspective. This article reviews various novel
systems for ophthalmic drug delivery.
The objective of this paper is to briefly review the
novel techniques for ophthalmic drug delivery so that
the pharmaceutical researchers get the concept of the
latest trends regarding this aspect.
THE END

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Techno ppt NOVEL DRUG DELIVERY SYSTEM

  • 1.
  • 3. Novel Drug delivery System (NDDS) refers to the approaches, formulations, technologies, and systems for transporting a pharmaceutical compound in the body as needed to safely achieve its desired therapeutic effects. •Advantages of Novel Drug Delivery System are: 1.Optimum dose at the right time and right location. 2.Efficient use of expensive drugs, excipients and reduction in production cost. 3.Beneficial to patients, better therapy, improved comfort and standard of living.
  • 5. Introduction Despite tremendous innovations in drug delivery, the oral route remains the preferred route for administration of therapeutic agents because of accurate dosage, low cost therapy, self medication, noninvasive method, and ease of administration leading to high level of patient compliance.
  • 8. • Molded tablets are prepared by forcing dampened powders under low pressure into die cavities. • Solidification depends upon crystal bridges built up during the subsequent drying process. • Molded tablets made from completely and readily water-soluble ingredients • They are employed orally, or where rapid drug availability is required such as in the case of Nitroglycerin Tablets, sublingually.
  • 9. Preparation of Molded Tablets • Molded tablets are prepared from mixtures of medicinal substances and a diluent usually consisting of lactose and powdered sucrose in varying proportions. • The powders are dampened with solutions containing high percentages of alcohol. • The dampened powders are pressed into molds, removed, and allowed to dry. • Molded tablets are quite friable and care must be taken in packaging and dispensing.
  • 10. Lyophilization • The drug is dissolved or dispersed in an aqueous solution of a carrier. • The mixture is poured into the wells of the preformed blister packs. • The trays holding the blister packs are passed through liquid nitrogen freezing tunnel to freeze the drug solution. • Then the frozen blister packs are placed in refrigerated cabinets to continue the freeze drying. • Finally the blisters are packaged and shipped. • Characteristics: The preparations are highly porous, have high specific surface area, dissolve rapidly and ultimately show improved absorption and bioavailability.
  • 11. STEPS INVOLVED IN LYOPHILIZATION FREEZING STAGE SECONDARY DRYING STAGE** * The temperature and pressure should be below the triple point of water i.e., 0.0098°C and 4.58mmHg. Easily removes moisture up to 98% to 99%. ** The temperature is raised to 50°C – 60°C and vacuum is lowered about 50mmHg. It takes about 10-20 hrs.
  • 12. Lyophilization • Advantage Water sensitive drug are prepared by this method as RDTs instead of dry- granulation (delay DT) • Disadvantage Some portion of drug remains in the wells of the blister packs EXAMPLES Loratidine (Claritin Reditab and Dimetapp Quick Dissolve) Cisapride monohydrate (Propulsid Quicksolv) Risperidone (Risperdal M-tab) Ibuprofen (Nurofen Flashtab)
  • 13. Direct Compression • A direct compression method uses conventional equipment, commonly available excipients, and a limited number of process steps. • The direct compression tablet's disintegration and solubilization are based on the single or combined action of super disintegrants, water-soluble excipients, and effervescent agents. • The choice of superdisintegrant for a tablet formulation depends largely on the nature of the drug being used. • TizanidineHCl,OxybutyninHCl,Rofecoxib,and Ethenzamide are some examples of model drugs that have been formulated as RDT by direct compression method.
  • 14. Super Disintegrants Used In Rapid Disintegrating Tablets
  • 15. Croscarmellose Sodium  Synonyms: (Ac-Di-Sol)  Cross linking makes it an insoluble, hydrophilic, highly absorbent material, resulting in excellent swelling properties and its unique fibrous nature gives it excellent water wicking capabilities.  Croscarmellose sodium provides superior drug dissolution and disintegration characteristics, thus improving bioavailability of formulations
  • 16. CROSPOVIDONE  Synonyms:- Crosslinked polyvinylpyrrolidone (PVP), Insoluble PVP, Polyvinylpolypyrrolidone (PVPP), Crospovidone , Crospovidonum  Crospovidone, NF, is a synthetic, insoluble but rapidly swellable, cross-linked homopolymer of N-vinyl-2-pyrrolidone
  • 17. Sodium Starch Glycolate  Synonyms: Carboxymethyl starch, Explotab, Primojel  Primojel promotes water penetration into the tablet and develops a disintegration force needed to push the particles apart.  High swelling capacity results in its high disintegration rate and efficiency.
  • 19. Pharmaceutical Lollipops • Lollipops have been used to deliver pharmaceuticals (chiefly, Lipophilic drugs) to patients. • Provide rapid absorption into the blood stream through the mucosa of the mouth • Absorption occurs much more rapidly than when drugs are swallowed and absorbed via the digestive system. • The dose can easily be controlled by administering the lollipop only until the desired effect is observed, thereby minimizing the dose • Lollipops provide a pleasant way for a reluctant patient to receive the pharmaceutical.
  • 20. Pharmaceutical Lollipops • In particular, lollipops containing the potent, short-acting narcotic fentanyl have been approved by the FDA for the treatment of severe pain. • For example: Actiq by Cephalon
  • 21. Fentanyl Lollipop • It is a solid formulation of fentanyl citrate on a plastic stick that dissolves slowly in the mouth for absorption across the buccal mucosa. • It is effective in treating cancer breakthrough pain and other problems, such as bone injuries, migraines, severe back pain, cluster headaches, neuropathy, arthritis, and moderate to severe chronic, non-malignant pain. • The dosage unit is a white, berry-flavored lozenge on a stick which is swabbed on the buccal mucosa, between cheek and gum to release the fentanyl quickly into the bloodstream.
  • 22. Fentanyl Lollipop Absorption •Normally 25% of the drug is absorbed via the buccal mucosa directly into the bloodstream while the remaining 75% is swallowed and then slowly absorbed in the gastrointestinal tract. •Two-thirds of the swallowed dose is metabolized by the liver and becomes unavailable •25% of the total dose will reach the bloodstream via the intestines •50% of the total dose will reach the bloodstream via both routes
  • 23. Fentanyl Lollipop Side effects •Sedation •Nausea •Constipation •tolerance •respiratory depression •dental decay •Each lozenge contains approx. 2grams of sugar, and has issues for pre-diabetic users and diabetic users.
  • 24. References • Fast disintegrating tablets: Opportunity in drug delivery system, Ved Parkash, Saurabh Maan, Deepika,Shiv Kumar Yadav, Hemlata, and Vikas Jogpal, J Adv Pharm Technol Res. 2011 Oct-Dec; 2(4): 223– 235. doi: 10.4103/2231-4040.90877 • Md.Nehal Siddiqui*, Garima Garg, Pramod Kumar Sharma, FAST DISSOLVING TABLETS: PREPARATION, CHARACTERIZATION AND EVALUATION: AN OVERVIEW, Volume 4, Issue 2, September – October 2010; Article 015,page 87-96 ISSN 0976 – 044X • System for delivering pharmaceuticals to the buccal mucosa , US 6103257 A, http://www.google.com/patents/US6103257 • https://en.wikipedia.org/wiki/Actiq
  • 26. TRANSDERMAL ROUTE • Transdermal patch is a medicated adhesive patch that is placed on skin to deliver a spacific dose of medication through skin & into the blood stream. • Attractive alternative to the conventional drug delivery methods of oral administration & injection.
  • 27. LATEST APPROACHES • Various technologies have been developed to by pass or modulate barrier function of skin.
  • 28. 1-IONTOPHORESIS • Effective & painless method of delivering medication to a localized tissue area by applying electrical current to a solution of the medication.
  • 29. 2-ELECTROPORATION • Intense electric charges create small pores in phospholipid bilayer of cell membranes can assist in transdermal delivery of drugs. • Appears to reversibly disrupt the lipid bilayers in stratum corneums & channels it creates are said to promote the passage of hydrophilic drugs through skin.
  • 30. 3-PHONOPHORESIS • Use of ultra sound of a suitable frequency to enhance skin permeability seems to be a useful alternative method for delivering drugs through skin & can be applied to vaccination & gene therapy. • Also known as sonophoresis.
  • 31. 4-MICRONEEDLES • Patches coated with hundreds of microscopic needles can deliver proteins, Nano particles & both small & large molecules through skin.
  • 33. Ophthalmic Preparations • Ophthalmic preparations are the specialized dosage forms designed to be instilled on to the external surface of the eye (topical) administered inside (intraocular) or adjacent (periocular) to the eye. • The most commonly employed ophthalmic dosages are:  Solutions  Suspensions  Ointments • The newest dosage forms for ophthalmic delivery are:  Gel-Forming Solutions(Situ Gels)  Ocular Inserts  Contact lenses with drugs
  • 34. Ophthalmic Preparations •Ophthalmic preparations are sterile products that are intended to be applied to the eyelids or placed in the space between the eyelids and the eyeball . •One of the problems associated with the use of ophthalmic solutions is the rapid loss of administered drug due to the blinking of the eye and the flushing effect of lacrimal fluids lost through tears.
  • 36. Ocular Inserts Inserts are solid or semisolid dosage forms without disadvantages of traditional ophthalmic drug forms . show the ability to stay in conjunctival sac for a longer period, and are more stable than conventional dosage forms. Polymeric materials most often employed in developing inserts include, for example, methylcellulose and its derivatives, that is, hydroxypropyl methylcellulose (HPMC) etc Advantages: Accurate dosing The possibility of slow substance release with constant speed Limiting its systemic absorption. Moreover, using them enables reduction of the drug application frequency, Decrease adverse effects and blurring of vision occurrence.
  • 37. Ocusert device • Example of this is the Ocusert Device for pilocarpine membrane-controlled delivery. • Pilocarpine is available in a membrane controlled reservoir system that is used in the treatment of glaucoma. • Pilocarpine is sandwiched between two EVA membranes. It also contains alginic acid, a seaweed carbohydrate, which serves as a carrier for Pilocarpine . • The small, clear device has a white annular border made of EVA copolymer impregnated with titanium dioxide (pigment) that makes it easier for the patient to see. • The insert is placed in the cul-de-sac, where it will float with the tears. The Pilocarpine will diffuse from the device and exert its pharmacologic effect
  • 38. Ophthalmic Inserts Lacrisert This medications is an insert that is placed in your eye to treat dry eye. It is usually used when an artificial tears solution is not successful. It is used to treat certain other eye disorders ( keratitis , decreased corneal sensitivity) Lacrisert is a rod-shaped watersoluble form of hydroxypropyl cellulose. The insert is placed in the inferior cul-de-sac of the eye once or twice daily for the treatment of dry eyes. The inserts soften and slowly dissolve it help in thickening the precorneal tear film and prolonging the tear film breakup.
  • 39. Gel-forming solutions They are semisolid viscous liquids, showing the ability to undergo sol- to-gel transitions when influenced by external factors, like appropriate pH, temperature, and the presence of electrolytes. This property causes slowing of drug drainage from the eyeball surface and increase of the active ingredient bioavailability. Polymers employed in developing these drug.
  • 40. Gel Extended Release Product • Certain preparations are designed to prolong the action of drug or to extend the action of drug • One example of these Ophthalmic Product in which viscosity increasing agents are used to increase the corneal contact time of drug i.e. • Timolol maleate ( Timoptic -XE, Merck) employs gellan gum which forms a gel upon contact with the precorneal tear film.
  • 41. Contact Lenses Coated with Drugs • . This drug form can absorb on its surface water- soluble substances, released after applying the drug over the eyeball for a longer period of time. The first and most widely used polymer in the production of lenses was the cross-linked poly (2-hydroxyethyl methacrylate) with small amount of ethylene glycol dimethylacrylate. • In recent years, research has been conducted on employing silicon-based lenses. Interest in contact lenses still grows. • Examples of drugs whose pharmaceutical availability from lenses was researched include timolol , ciprofloxacin , dexamethasone , and cyclosporine .
  • 43. Definition • Implants are small sterile solid masses consisting of a highly purified drug (with or without occupants) made by compression or molding or extrusion. • Implants are drug delivery systems which provide controlled delivery of drug over a period of time at the site of implantation
  • 44. Introduction • Implants are intended for implantation in the body (usually subcutaneously) for the purpose of providing continuous release of the drug over long periods of time. • Implants are administered by means of a suitable special injector or surgical incision. • These are developed with a view to transmit drugs and fluids into the blood stream without the repeated insertion of needles • These systems are particularly suited for delivery requirements of drugs such as insulin, steroids, antibiotics, analgesics, heparin, total parenteral nutrition etc.
  • 46. Advantages Unattended continuous delivery within the therapeutic window Avoids the highly variable peak and trough concentrations Enhanced drug efficacy Minimized side effects Termination of therapy as and when required Patient compliance is also a benefit of continuous dosing with these implants as they operate for a long period of time once implanted
  • 47. Disadvantages The reaction between host and implant. Implantation procedure is difficult in the case of larger implants. Inadequate release. Requires small surgery for large implantation & painful.
  • 48. Application A. Cancer Treatment Gliadel Wafer: Delivers carmustine for the treatment of brain tumours directly at the site of tumour to prevent reccurrence of tumours. Depocyte: cytarabine releasing implantable DDS used to treat acute leukemia. Duros osmotic pump: Non-biodegradable implantable DDS used to deliver Leoprolide acetate in the treatment of prostate cancer. B. Osteoporosis Micro chips: This device made by ELI Lilly & coworkers used to deliver Forteo drug used to increase bone density in patients suffering from severe osteoporosis.
  • 49. D. Contraceptives Norplant: delivers Norgestrol to achive contraception. Reactions of host to implant: Changes in permeability of polymer to body fluids. Environmental stress cracking. Chemical breakdown of polymeric material. Loss of tensile strength in case of hydrophobic polymers. C. Ocular Diseases Lacrimedics: these are collagen implants used to treat dry eye syndrome by partially blocking tear removing canals and they dissolve within 7-10 days. Vitrasert: delivers ganicyclovir used to treat AIDS related retinitis.
  • 51. Novel concept in vaginal drug delivery • NVDDS are designed with desirable distribution, bio adhesive, retention and release characteristic.
  • 52.
  • 53. ADVANTAGES • Ease of administration • Reduce side effects • Avoids first pass metabolism • Effective for orally inactive drugs • High vascularization • Low enzymatic activity.
  • 54. DISADVANTAGES • Local irritation of some drugs • Personal hygiene • Gender specificity • Influence of sexual intercourse • Cultural sensitivity • Some of drugs are sensitive to vaginal pH. 37
  • 55. RECENT ADVANCES IN VAGINAL DRUG DELIEVRY Achieved by the use of • bio adhesive and • other novel delivery system
  • 56. Bio adhesives delivery systems Bio adhesive vaginal formulations that are capable of delivering the active agent for an extended period at a predictable rate
  • 57. Other novel delivery systems • Phase change polymers • Formulations based on a thermoplastic graft co polymer
  • 58. Evaluation Of Vaginal Formulations • In Vitro studies • In vivo studies Recent developments • Effervescent vaginal tablets of nystatin • Bio adhesive effervescent ketoconazole tablets
  • 59. APPLICATIONS OF INTRA VAGINAL DRUG DELIEVERY SYSTEM • Vaginal immunization • Treatment of HIV infection • Treatment of local fungal infection • Delievery of hormones • Multi-cycle administration of vaginal contraceptive rings
  • 60. Vaginal ring Vaginal rings are 'doughnut-shaped' polymeric drug delivery devices designed to provide controlled release of drugs to the vagina over extended periods of time. Several vaginal ring products are currently available, including: Femring : a low-dose estradiol-acetate releasing ring, manufactured from silicone elastomer, for the relief of hot flashes and vaginal atrophy associated with menopause. NuvaRing: a low-dose contraceptive vaginal ring, releasing progesterone and estrogen. 60
  • 61. ZABAB KHAN 131066 URETHRAL ROUTE OF ADMINISTRATION
  • 62. URETHRAL ROUTE OF ADMINISTRATION • The urethral route of administration is application of drug by insertion into the urethra • Common dose forms include: ◦ solutions ◦ suppositories • Urethral delivery may be used to treat ◦ incontinence ◦ impotence in men • Disadvantages ◦ inconvenience ◦ localized pain
  • 63.
  • 64. ALPROSTRADIL URETHRAL MICROSUPPOSITORY • Single used • 1.4 mm in diameter and 3-6mm in length • Strengths available: 125,150,250,500 and 1000 microgram/units • Inserted with the help of device • Suspended in PEG • Self insert and removal • Sustain delivery for 4-7days
  • 66. PHARMACEUTICS & NOVEL DRUG DELIVERY SYSTEMS Tariq Jamshaid Surge Laboratories Private Limited, Pakistan
  • 67. Novel Drug delivery System (NDDS) refers to the approaches, formulations, technologies, and systems for transporting a pharmaceutical compound in the body as needed to safely achieve its desired therapeutic effects. It may involve scientific site-targeting within the body, or it might involve facilitating systemic pharmacokinetics; in any case, it is typically concerned with both quantity and duration of drug presence. Novel Drug delivery is often approached via a drug's chemical formulation, but it may also involve medical devices or drug-device combination products. Drug delivery is a concept heavily integrated with dosage form and route of administration. NDDS is advanced drug delivery system which improves drug potency, control drug release to give a sustained therapeutic effect, provide greater safety, finally it is to target a drug specifically to a desired tissue. NDDS is a system for delivery of drug other than conventional drug delivery system. NDDS is a combination of advance technique and new dosage forms which are far better than conventional dosage forms. Advantages of Novel Drug Delivery System are: 1. Optimum dose at the right time and right location. 2. Efficient use of expensive drugs, excipients and reduction in production cost. 3. Beneficial to patients, better therapy, improved comfort and standard of living. Basic modes of novel drug delivery systems are: 1. Targeted Drug Delivery System 2. Controlled Drug Delivery System 3. Modulated Drug Delivery System Factors affecting the design of controlled release products are: 1. Physicochemical properties of a drug 2. Route of administration 3. Acute/Chronic therapy 4. Target sites 5. The Patient 6. The disease state/leve.
  • 68. CURRENT TRENDS IN NOVEL OPHTHALMIC DRUG DELIVERY SYSTEM: AN OVERVIEW Sidra Farooq, Mirza Yasir Hussain and Syed Muhammad Farid Hassan Department of Pharmaceutics, Faculty of Pharmacy, University of Karachi, Main University Road, Karachi
  • 69. One of the most daring tasks faced by the pharmaceutical researchers is the ophthalmic drug delivery. Their aim is to achieve and sustain a therapeutic level at the site of action for extended period of time. Therefore, to withstand drug levels at the target site for a sufficient time, novel drug delivery techniques are developed. Ophthalmic drug delivery route has seen significant advancement for future perspective. This article reviews various novel systems for ophthalmic drug delivery. The objective of this paper is to briefly review the novel techniques for ophthalmic drug delivery so that the pharmaceutical researchers get the concept of the latest trends regarding this aspect.
  • 70.