This document discusses different types of activation modulated drug delivery systems (DDS). It describes DDS that are activated by physical, chemical, or biological means. Some examples of physically activated DDS include osmotic pressure-activated, hydrodynamic pressure-activated, vapour pressure-activated, and mechanically activated systems. Magnetically activated and sonophorosis activated DDS are also mentioned. The document provides details on the mechanisms and equations for rate of drug release for some of these systems. It further discusses iontophoresis-activated and hydration-activated DDS and provides one example for each.
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
rate control drug delivery system machenism Nirmal Maurya
rate control drug delivery system
including all machenism with figures
Prepared by
NIRMAL MORYA
M.Pharma
Mob +91 7060346038
BBAU Lucknow
A Central University
These systems are capable of controlling the rate of drug delivery, sustaining the duration of therapeutic efficacy, and/or targeting the delivery of drug to a tissue. Depending upon the technical sophistication, these rate-control drug delivery systems can be classified into three major categories: (i) pre-programmed drug delivery, (ii) activation-controlled drug delivery, and (iii) feedback-regulated drug delivery.
Implants are cylindrical, monolithic devices of millimeter or centimeter dimensions, implanted into the subcutaneous or intramuscular tissue by an minor surgical incision or injected through a large bore needle; and release the incorporated drug in a controlled manner, allowing the adjustment of release rates over extended periods of time, ranging from several days up to one year.
Implantable Drug Delivery Systems: Delivering Medication on Demand
Implantable drug delivery systems (IDDS) are miniature devices surgically placed under the skin or inside tissues to deliver a sustained and controlled release of medication directly to the target site. This targeted approach offers several advantages over traditional oral or injectable medications:
Benefits:
Improved treatment compliance: Eliminates the need for frequent dosing, improving adherence to treatment plans.
Enhanced efficacy: Delivers drugs directly to the site of action, maximizing their therapeutic effect.
Reduced side effects: Minimizes systemic exposure to the drug, potentially reducing unwanted side effects.
Controlled release: Offers precise control over the release rate and duration of medication delivery, optimizing treatment effectiveness.
Long-term therapy: Can provide continuous medication delivery for months or even years, ideal for chronic conditions.
Types of IDDS:
Biodegradable implants: Made from materials that naturally degrade over time, releasing the drug at a predetermined rate.
Non-biodegradable implants: Composed of materials that remain in the body after the drug is released, requiring surgical removal.
Reservoir implants: Contain a pre-filled reservoir of medication released through a controlled mechanism.
Pump implants: Use a micro-pump to deliver the medication at specific intervals or in response to external stimuli.
Applications:
Pain management: Chronic pain, post-surgical pain, arthritis
Hormonal therapy: Contraception, hormone replacement therapy
Cancer treatment: Localized chemotherapy, targeted drug delivery
Psychiatric disorders: Depression, schizophrenia
Neurological disorders: Parkinson's disease, epilepsy
Challenges and considerations:
Surgical implantation: Requires a minor surgical procedure, carrying associated risks and potential complications.
Cost: The devices and implantation procedure can be expensive.
Limited drug suitability: Not all medications are compatible with IDDS technology.
Device failure: Mechanical malfunctions or material degradation can occur over time.
Future of IDDS:
Advancements in materials science, miniaturization, and biocompatibility are paving the way for more sophisticated IDDS with:
Closed-loop systems: Sensors monitoring disease markers and adjusting drug release in real-time.
Multifunctional capabilities: Combining drug delivery with other functionalities like disease monitoring or biostimulation.
Personalized medicine: Tailored IDDS designed for individual patient needs and genetic profiles.
Recent Advances in Colon Targeted Drug Delivery SystemDarshil Shah
Colon Targeted Drug delivery is the most convenient and desirable drug targeting method for the drugs which degrades in acidic environment, and also preferable for prolong or delayed release and also desease specisic to colon.
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2. CLASSIFICATION
Rate pre-programmed drug delivery systems
Activation – modulated drug delivery systems
Feedback- regulated drug delivery systems
Site- targeting drug delivery systems
2
3. ACTIVATION MODULATED DDS
Drug delivery is activated and controlled by physical,
chemical or bio-chemical processes or facilitated by the
energy supplied externally
Classification of activation modulated DDS
Based on the nature of the process applied or the type
of energy used
1. Physical means
2. Chemical means
3. Biological means
3
4. DDS activated by physical means
a. Osmotic pressure- activated DDS
b. Hydrodynamic pressure activated DDS
c. Vapour pressure activated DDS
d. Mechanically activated DDS
e. Magnetically activated DDS
f. Sonophorosis activated DDS
g. Iontophoresis activated DDS
h. Hydration activated DDS
4
5. 1. Osmotic pressure- activated DDS
drug reservoir can be a solution contained within an
impermeable collapsable tube.
This is covered with osmotic agent place in a rigid semi
permeable housing with controlled water permeability.
The rate of drug release is modulated by the gradient of
osmotic pressure.
Q/t = PwAm (πs-πe) /hm
Pw = water permeability
Am = effective surface area
hm =thickness of the semi permeable housing
5
7. 2. Hydrodynamic pressure activated DDS
hydrodynamic pressure is used as the source of energy
to activate the drug release.
7
8. Q/t = Pf Am/hm (θs – θe)
Pf = fluid permeability
Am = effective surface area
hm = thickness of the wall with annular openings
θs – θe = difference in hydrodynamic pressure between the
DDS and the environment
8
9. 3. Vapour pressure- activated drug delivery systems
Drug inside infusion compartment is separated from
pumping compartment by freely movable partition.
Pumping compartment contains a fluorocarbon
fluid that vaporizes at body temperature
The vapour pressure created moves the partition
upward, forcing the drug to be delivered.
Eg: INFUSAID implants (heparin)
9
11. Q/t= d4(Ps-P-e)/40.74µl
d & l = the inner diameter and the length of the delivery
cannula, respectively
Ps-P-e = difference between the vapour pressure in the
pumping compartment and the site of
implantation.
µ = viscosity of the drug formulation used.
11
12. 4. Mechanically activated drug delivery system
Equipped with a mechanically activated pumping system
A measured dose of drug formulation is reproducibly
delivered
The volume of solution delivered is controllable, as small as
10-100µl
Volume of solution delivered is independent of the force &
duration of activation applied as well as the solution volume
in the container.
Example is the development of metered dose nebulizer for
the intranasal administration of a precision dose of buserelin
(LHRH).
12
14. 5. Magnetically activated drug delivery systems
Drug reservoir is a dispersion of peptide or protein
powders in a polymer matrix
Low rate of delivery is improved by incorporating
electromagnetically triggered vibration mechanism
14
15. Coating polymer can be a ethylene-vinyl acetate
copolymer or silicon elastomers.
These systems have been used to deliver protein drugs,
such as bovine serum albumin
6. Sonophoresis-activated drug delivery systems
Utilize ultrasonic energy to activate the delivery of the
drugs from a polymeric drug delivery device
can be fabricated from either a non degradable
polymer, such as ethylene-vinyl acetate copolymer,
a bio erodible polymer such as poly[bis(p-
carboxyphenoxy)alkane anhydride].
15
17. 7. Iontophoresis-activated drug delivery systems
uses electrical current to activate and to modulate
the diffusion of a charged drug molecule across
the skin in a facilitated rate
17
18. skin permeation rate of a charged molecule i consist of 3
components
Jiisp = Jp+Je+Jc
Jp = passive skin permeation flux
Je = electrical current driven permeation flux
Jc = convection flow-driven skin permeation flux
IONSYS - fentanyl iontophoretic transdermal system
Example : development of an iontophoretic DDS of
dexamethasone sodium phosphate
18
19. 8. Hydration-activated drug delivery system
Depends on the hydration induced swelling process to
activate the release of drug
Drug reservoir is homogeneously dispersed in a swellable
polymer matrix fabricated from a hydrophilic polymer
Release of the drug is controlled by the rate of swelling of
the polymer matrix.
Example is VALRELEASE tablet- diazepam in hydrocolloid
and pharmaceutical excipients.
In stomach absorbs the gastric fluid & forms colloidal gel
that starts from the tablet surface and grows inward.
19
20. release of the drug is controlled by matrix diffusion
through this gel barrier
20
21. REFERENCES
NOVEL DRUG DELIVERY SYSTEMS, 2nd edition, Yie W.
Chien
CONTROLLED DRUG DELIVERY- FUNDAMENTALS AND
APPLICATIONS, 2nd edition, edited by Joseph R.
Robinson and Vincent H. L. Lee
http://www.rxlist.com/ionsys-drug.htm
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