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DRUG CARRIER
DELIVERY SYSTEM.
PREPARED BY
Dhara Patel
CONTENTS :
INTRODUCTION ON DRUG CARRIER SYSTEM.
TYPES OF DRUG CARRIER SYSTEM.
PARTICULATE CARRIER.
TYPES OF PARTICULATE CARRIER.
PURPOSES FOR DEVELOPMENT OF
PARTICULATE CARRIER SYSTEMS.
LIMITATIONS.
VESICULAR DRUG DELIVERY SYSTEM.
REFERENCES.
2
INTRODUCTION :
• What is drug ?
A medicine or other substance which has a
physiological effect when ingested or otherwise
introduced into the living body.
Synonyms :
Medicine, medical drug, medication, medicament. And many other.
• What is drug carrier ?
A drug carrier is any substrate used in the process of drug
delivery which serves to improve the selectivity,
effectiveness, and/or safety of drug administration.
3
DRUG CARRIER PROCESS :
4
Particulate Carrier :
• Drug carriers achieve different goals : bioavailability,
stability, preventing the drug interactions.
• Here it is describes unique nature and applications.
• Developed for various purposes depending on the
needs.
• Different from each other structure, characteristics,
composition manufacturing procedure
5
PARTICULATE CARRIER TYPES :
6
1)Microspheres :
Free flowing powders : Consisting of proteins, synthetic
polymers.
Biodegradable in nature.
Particle size less than 200μm.
Developed using different methods : emulsion techniques,
polymerization techniques, spray drying, solvent evaporation.
 Applications : Controlled drug delivery, vaccine delivery.
Much Attention : Targeting of anticancer drugs to the
tumour.
Diagnostics, gene & genetic materials, safe targeted and
effective in vivo delivery and supplements.
7
Example of Microspher :
Name of drug : SIR – Sphere
Use : In radiation therapy , In liver tumor ( cancer )
8
2)Multicomposite Capsules :
Self assembling ultrathin multilayered capsule.
layer-by-layer adsorption colloidal particles.
Called as : Biomimic capsule.
Multilayer films of organic compounds on solid
surface .
Adsorption :Polyanions and Polycations
Extended to other materials such as proteins or
colloids
9
International journal of pharmaceutics.
10
Example of Multicomposite Capsule :
 Composite use in : Multivitamins, multi-minerals, and Zinc
supplements.
Use : loss of appetite, fatigue, or general debility. Helps
improve growth, strength and vitality.
11
3)Nanoparticles :
 Particulate dispersions or solid particles.
 Size in the range of 10-1000nm.
-- dissolved, entrapped, encapsulated or attached to a
nanoparticle matrix.
 Drug is confined to a cavity surrounded by a unique polymer
membrane.
 Matrix systems.
 Coated :hydrophilic polymer such as poly(ethylene glycol)
(PEG) .
-- long-circulating particles.
12
Formulation and intestinal absorption enhancement evaluation of water-
in-oil microemulsions incorporating medium-chain glycerides
Continue….
Prepared by three methods :
(1) dispersion of preformed polymers;
(2) polymerization of monomers; and
(3) ionic gelation or co-acervation of hydrophilic
polymers.
Use :
-- potential drug delivery devices because of their
ability to circulate for a prolonged period time in
systemic circulation.
-- target a particular organ.
-- carriers for DNA in gene therapy.
-- capable in delivering the proteins, peptides, genes.
13
14
Example of Nanoparticle :
 Real natural product, without chemical, composed only of small
particles suspended in pure water.
 Use : natural substance with antibiotic properties, antibacterial,
antiviral, antifungal and anti-inflammatory.
15
4)Aquasomes :
“bodies of water” : water like properties help to
protect and preserve the biological molecules.
Oligo-meric film : drug moieties, bio-chemically active
molecules --adsorbed with or without modification.
Three layered structures : non-covalent and ionic
bonds.
Three steps : preparation of core, coating of core and
immobilization of drug molecule.
Delivery of vaccines, haemoglobin, drugs, dyes,
enzymes and even gastric material.
16
Wang N., Wu X. S., Preparation and characterization of agarose hydrogel
nanoparticles for protein and peptide drug delivery.,
5)Liposomes :
 microscopic vesicles : one or more concentric lipid bilayers,
separated by water or aqueous buffer.
 diameter : 25-100μm.
 Small Unilamellar Vesicles (SUV) (10-100 nm)
 Large Unilamellar Vesicles (LUV) (100-3000 nm).
 More than one bilayers Multilamellar Vesicles (MLV).
 different methods : film hydration technique, ether injection
method, reverse phase evaporation method, membrane
extrusion technique .
 all routes, and can be used as carrier for all drugs
17
Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.Int J Pharm Life .
Liposome of drug delivery :
18
Example of Liposome :
Duxorubicin.
Use : Blood cancer
19
6)Lipid Emulsions :
Heterogenous dispersions of two immiscible liquids (oil-
in-water or water-in oil) .
Aggregation, flocculation, coalescence.
Separation : second law of thermodynamics.
0il-in-water (o/w), water-in-oil (w/o), micron, submicron
and double or multiple emulsions (o/w/o and w/o/w).
Colloidal drug carriers : therapeutic applications.
20
6. ConstantinidsP.P., Scalart J.P., Lancastar S., Marcello
J.,MarksG.,EllenH.,Smith P.L.,
21
Example :
Ingredient :Amino acid ,
Sorbitol
Total Parenteral Nutrition (TPN) therapy.
22
PURPOSES FOR DEVELOPMENT
 Can target the different organs to produce desired action without
causing harm to the other healthy organs.
 Enhances the bioavailability of the drugs administered orally
by avoiding first pass metabolism
 Enhances the drug absorption
 They enhance the solubility of poorly soluble drugs.
 Deliver vaccines.
 Improve the stability of the drugs.
 Large molecular weights like proteins, peptides can be
administered through these carrier sysem.
 Target particular organs in the body.
23
International journal of pharmaceutics
LIMITATIONS :
Sometimes, these carriers will exhibit the dose
dumping.
These are associated with problems like storage,
leaching, aggregation.
Extra care should be taken while
manufacturing these carriers.
Expensive.
24
International journal of pharmaceutics
Vesicular drug delivery systems:
Deliver the drug at a rate directed by need of
body during the period of treatment, and channel
the active entity to the site of action.
Various routes of administration, to achieve
targeted and controlled drug delivery .
Improves the therapeutic efficacy and reduces the
side effects.
Targeting means the delivery of drugs to receptor,
organs or any other specific part of body to which
one wishes to deliver the entire drug .
25
Deliver the drug at target site; these include
immunoglobulins, serum proteins, synthetic
polymers, microspheres, liposomes, niosomes,
erythrocytes .
Improve : Therapeutic index, solubility, stability
and rapid degradation of drug molecules.
26
Continue…
umar R, Kumar S, Jha SS, Jha AK. Vesicular system-carrier
for drug
delivery.
Types:
Lipoidal bio-carriers for site specific targeting
1. Liposomes 5. Sphingosomes
2. Emulsomes 6. Transferosomes
3. Enzymosomes 7. Pharmacosomes
4. Ethosomes 8. Virosomes
Non- lipoidal biocarriers for site-specific
targeting
1. Niosomes 3. Aquasomes
2. Bilosomes
27
1] Liposomes :
 20 nanometers to several micrometers in size.
 Lipid bilayer structures.
 Enclosed by a membrane, composed of lipid molecules :both
hydrophilic and lipophilic drugs can be successfully entrapped.;
within bilayer membrane.
 Hydrophilic drugs get entrapped in the central aqueous core of the
vesicles.
 Attach to cellular membrane :fuse with them, releasing their
content into the cell.
 Drug trapped inside is released.
28
Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.
2] Emulsomes :
 Lipid based drug delivery system .
parenteral delivery of drugs having poor aqueous solubility.
 Internal core is made up of fats and triglycerides,
stabilized : o/w emulsion , addition of high concentration of
lecithin.
 Characteristics of both liposomes and emulsions.
 Solidified or semi solidified internal oily core : better
opportunity to load lipophilic drugs in high concentration.
 Enhanced drug delivery.
 Improved preclinical efficacy for oral route.
29
Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.
3 ]Enzymosomes:
 proteins like enzymes :delivered through several approaches.
Like polymeric carriers; aqueous space of lipid and bilayered
vesicles.
But delivery by attachment on surface of liposomes has shown the
prominent response for the development of antibodies at the target
site.
 Enzymes upon complexing with lipids : enzymosomes.
 developed with long circulation time in the blood.
 accumulate at inflammed target sites.
 maintaining enzymatic activity in its intact form .
30
Example :
 Milk or dairy product
 Use : digest-protein product
31
4] Ethosomes :
 Developed for delivering the drugs having low penetration
power through skin.
Soft lipid vesicles : size range from tens of nanometers to microns.
 containing phospholipids, alcohol : high concentration and
water.
 Better skin permeation ability.
 Surface negative net charge to ethosomes due to which size of
vesicles decreases.
 Used for delivery of various antifungal agents, antiviral agents.
 Pharmacological efficacy in drug targeting :
transdermal and dermal sites for the treatment of
various skin diseases.
32
Gangwar S, Singh S, Garg G. Ethosomes: a novel tool for drug
delivery through skin
Example :
33
5] Sphingosomes
 Introduced to overcome the stability problems of liposomes.
 Presence of sphingolipids instead of phospholipids present in
liposomes.
 Used : liposomes are prone to undergo chemical
Degradation. : oxidation and hydrolysis of ester linkage.
 Targeting of the drug to the site of action, because of being
biodegradable,
 Targeting to tumour tissues: site-specific ligands to
achieve active targeting.
 Better drug retention.
 Ability to benefit from this novel encapsulation.
34
Samad A, Sultana Y, Aqil M. Liposomal systems: an update review.
Curr Drug Deliv.
Example : 35
6] Transferosomes :
 Transferosome means carrying body.
 Squeeze itself through a pore, smaller than its size owing to its
elasticity,
 Enhance the skin penetration and deliver the drug non-
invasively through the skin barrier .
 Used : as carrier, controlled and targeted delivery of proteins,
peptides, hormones, oral delivery of peptides likeinsulin and
interferons.
 10 timeÊs higher concentration in tissues under skin.
 Anti-ovulatory effect as compared to plain drug for oral
administration.
36
Sivasankar M, Katyayani T. Liposomesthe future of formulations. Int J Res Pharm
Chem
Example :
37
7] Pharmacosomes
Pharmacosomes are novel vesicular drug delivery systems
having unique advantages over other drug delivery systems .
Provides maximum entrapment efficiency.
The three main components for the preparation of
pharmacosomes are : drug, solvent and lipid.
Drug should contain active hydrogen atom , esterified with
lipid and form amphiphilic complexes, which facilitate
membrane transfer.
38
soft hybrid biocarriers of supramolecular construction for drug
delivery.
8] Virosomes :
Reconstituted viral envelopes .
Lipid bilayer , inserted viral glycoproteins.
Different enveloped viruses.
Liposomes with influenza virus hemagglutinin (HA) and
neuraminidase (NA) spikes on their surface.
Retain the cell entry and membrane fusion.
 Use : vaccination for the efficient induction of antibody
responses against the virus they are derived from .
39
World Journal pharmacy and pharmaceutical science
Example :
40
Non-LipoidalBiocarriers for
Site-Specific Targeting
41
1] Niosomes:
Vesicles on hydration of mixture of cholesterol and a single
alkyl chain nonionic and non-toxic surfactant.
Number of non-ionic surfactants have been used to prepare
vesicles.
Eg :., polyglycerol
alkyl ethers, glucosyldialkyl ethers, crown ethers,and a series
of spans and tweens.
Vesicles are termed as niosomes.
10-1000nm consisting of spherical, uni or multilamellar and
polyhedral vesicles in aqueous media.
42
World Journal pharmacy and pharmaceutical science
Example :
 Use : Mackup base
43
2] Bilosomes :
 Novel innovative drug delivery carriers : deoxycholic acid
incorporated into the membrane of niosomes.
 Bile salt stabilized vesicles are known as bilosomes.
 Therapeutic efficacy of drugs : stability in gastro intestinal tract.
 Increase the bioavailability of drugs .
 Liver and release the drug, so found to be an effective tool in
drug targeting to liver.
 Found to stabilize : vesicles in GI environment.
44
. Formulation and characterization of vesicular drug delivery system for
anti-HIV drug
Example :
45
3] Aquasomes
 One of the most recently developed delivery system for
bioactive molecules.
 Aquasomes are three layered structures.
(core, coating and drug)
 Self-assembled through non covalent bonds, ionic bonds and
vanderwaals forces.
 Aquasomes are spherical 60- 300nm size particles .
 Aquasomes can be used as red blood cell substitutes. :
release of oxygen by haemoglobin.
46
Functionalized nanocarriers to image and target fungi infected cells.
Example :
 Used as vaccines for delivery of viral antigen, targeted intracellular gene
therapy, for delivery of insulin and enzymes like DNAase and
pigments/dyes .
47
Summary:
 Drug delivery research areas is continuously broaden and modified as a
results of the realization of many factors (such as poor drug solubility and/or
absorption, rapid metabolism, high fluctuation in the drug plasma level and
variability) adversely affect in-vivo results, in conventional drug delivery
system.
 Lipids are one of the basic building blocks of biological membranes.
 Nanoscale-based delivery strategies are beginning to make a significant
impact on global pharmaceutical planning and marketing.
 Among the approaches for exploiting nanotechnology developments in
medicine, various nanoparticulates offer some unique advantages as
pharmaceutical carriers in delivery systems and image enhancement agents.
 The review illustrates the various classes of particulate lipid-based carriers
among them; lipoproteins, lipid nanoparticles either; solid lipid nanoparticles,
nanostructured lipid carriers, or lipid drug conjugates, lipid nanocapsules,
and liposomes.
 Lipid-based particulate carriers’ applications in various areas were also
addressed.
48
Refrence:
 International Journal of pharmacy ; Review article
by :Department of pharmaceutics, Pullareddy institute of
pharmacy,Andhrapradesh,India
 .World Journal pharmacy and pharmaceutical science ,Teegala Ram
Reddy College of Pharmacy, Meerpet Hyderabad, Telangana- India.
 .Bhadra D , Gupta G , Bhadra S, Umamaheshwari RB , Jain N .
,Multicomposite ultrathin capsules for sustained ocular delivery of
ciprofloxacin hydrochloride, J Pharm Pharm Sci. 2004 ; 16: 7(2):241-51
 .Manish G, Vimukta S. Targeted drug delivery system: a review. Res J
Chem Sci. 2011; 1(2):135-138.
49
 Kumar R, Kumar S, Jha SS, Jha AK. Vesicular system-carrier for drug
delivery. Der Pharmacia Sinica. 2011; 2(4):192-202.
 Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.Int J Pharm
Life Sci. 2011; 2(7): 945-951.
 Wagner A, Uhl KV. Liposome technology for industrial purposes.J Drug
Deliv. 2011; 2011:1-9.
 Sivasankar M, Katyayani T. Liposomesthe future of formulations. Int J Res
Pharm Chem. 2011; 1(2):259-267.
 Lehtinen J, Raki M, Bergstrom KA, Uutela P, Lehtinem K, Hiltunen A,
Pikkarainen J, Liang H, Pitkanen S, Maatta AM, Ketola RA, Yliperttula M,
Wirth T, Urtti A. Pre-targeting and direct immunotargeting of liposomal
drug carriers to ovarian carcinoma. Plosone. 2012; 7(7):1-10.
 Doijad RC, Bhambere DS, Manvi FV, Deshmukh NV. Formulation and
characterization of vesicular drug delivery system for anti-HIV drug. J
Global Pharm Technol. 2009; 1(1):94100
50
51

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Drug carrier delivery system

  • 2. CONTENTS : INTRODUCTION ON DRUG CARRIER SYSTEM. TYPES OF DRUG CARRIER SYSTEM. PARTICULATE CARRIER. TYPES OF PARTICULATE CARRIER. PURPOSES FOR DEVELOPMENT OF PARTICULATE CARRIER SYSTEMS. LIMITATIONS. VESICULAR DRUG DELIVERY SYSTEM. REFERENCES. 2
  • 3. INTRODUCTION : • What is drug ? A medicine or other substance which has a physiological effect when ingested or otherwise introduced into the living body. Synonyms : Medicine, medical drug, medication, medicament. And many other. • What is drug carrier ? A drug carrier is any substrate used in the process of drug delivery which serves to improve the selectivity, effectiveness, and/or safety of drug administration. 3
  • 5. Particulate Carrier : • Drug carriers achieve different goals : bioavailability, stability, preventing the drug interactions. • Here it is describes unique nature and applications. • Developed for various purposes depending on the needs. • Different from each other structure, characteristics, composition manufacturing procedure 5
  • 7. 1)Microspheres : Free flowing powders : Consisting of proteins, synthetic polymers. Biodegradable in nature. Particle size less than 200μm. Developed using different methods : emulsion techniques, polymerization techniques, spray drying, solvent evaporation.  Applications : Controlled drug delivery, vaccine delivery. Much Attention : Targeting of anticancer drugs to the tumour. Diagnostics, gene & genetic materials, safe targeted and effective in vivo delivery and supplements. 7
  • 8. Example of Microspher : Name of drug : SIR – Sphere Use : In radiation therapy , In liver tumor ( cancer ) 8
  • 9. 2)Multicomposite Capsules : Self assembling ultrathin multilayered capsule. layer-by-layer adsorption colloidal particles. Called as : Biomimic capsule. Multilayer films of organic compounds on solid surface . Adsorption :Polyanions and Polycations Extended to other materials such as proteins or colloids 9 International journal of pharmaceutics.
  • 10. 10
  • 11. Example of Multicomposite Capsule :  Composite use in : Multivitamins, multi-minerals, and Zinc supplements. Use : loss of appetite, fatigue, or general debility. Helps improve growth, strength and vitality. 11
  • 12. 3)Nanoparticles :  Particulate dispersions or solid particles.  Size in the range of 10-1000nm. -- dissolved, entrapped, encapsulated or attached to a nanoparticle matrix.  Drug is confined to a cavity surrounded by a unique polymer membrane.  Matrix systems.  Coated :hydrophilic polymer such as poly(ethylene glycol) (PEG) . -- long-circulating particles. 12 Formulation and intestinal absorption enhancement evaluation of water- in-oil microemulsions incorporating medium-chain glycerides
  • 13. Continue…. Prepared by three methods : (1) dispersion of preformed polymers; (2) polymerization of monomers; and (3) ionic gelation or co-acervation of hydrophilic polymers. Use : -- potential drug delivery devices because of their ability to circulate for a prolonged period time in systemic circulation. -- target a particular organ. -- carriers for DNA in gene therapy. -- capable in delivering the proteins, peptides, genes. 13
  • 14. 14
  • 15. Example of Nanoparticle :  Real natural product, without chemical, composed only of small particles suspended in pure water.  Use : natural substance with antibiotic properties, antibacterial, antiviral, antifungal and anti-inflammatory. 15
  • 16. 4)Aquasomes : “bodies of water” : water like properties help to protect and preserve the biological molecules. Oligo-meric film : drug moieties, bio-chemically active molecules --adsorbed with or without modification. Three layered structures : non-covalent and ionic bonds. Three steps : preparation of core, coating of core and immobilization of drug molecule. Delivery of vaccines, haemoglobin, drugs, dyes, enzymes and even gastric material. 16 Wang N., Wu X. S., Preparation and characterization of agarose hydrogel nanoparticles for protein and peptide drug delivery.,
  • 17. 5)Liposomes :  microscopic vesicles : one or more concentric lipid bilayers, separated by water or aqueous buffer.  diameter : 25-100μm.  Small Unilamellar Vesicles (SUV) (10-100 nm)  Large Unilamellar Vesicles (LUV) (100-3000 nm).  More than one bilayers Multilamellar Vesicles (MLV).  different methods : film hydration technique, ether injection method, reverse phase evaporation method, membrane extrusion technique .  all routes, and can be used as carrier for all drugs 17 Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.Int J Pharm Life .
  • 18. Liposome of drug delivery : 18
  • 19. Example of Liposome : Duxorubicin. Use : Blood cancer 19
  • 20. 6)Lipid Emulsions : Heterogenous dispersions of two immiscible liquids (oil- in-water or water-in oil) . Aggregation, flocculation, coalescence. Separation : second law of thermodynamics. 0il-in-water (o/w), water-in-oil (w/o), micron, submicron and double or multiple emulsions (o/w/o and w/o/w). Colloidal drug carriers : therapeutic applications. 20 6. ConstantinidsP.P., Scalart J.P., Lancastar S., Marcello J.,MarksG.,EllenH.,Smith P.L.,
  • 21. 21
  • 22. Example : Ingredient :Amino acid , Sorbitol Total Parenteral Nutrition (TPN) therapy. 22
  • 23. PURPOSES FOR DEVELOPMENT  Can target the different organs to produce desired action without causing harm to the other healthy organs.  Enhances the bioavailability of the drugs administered orally by avoiding first pass metabolism  Enhances the drug absorption  They enhance the solubility of poorly soluble drugs.  Deliver vaccines.  Improve the stability of the drugs.  Large molecular weights like proteins, peptides can be administered through these carrier sysem.  Target particular organs in the body. 23 International journal of pharmaceutics
  • 24. LIMITATIONS : Sometimes, these carriers will exhibit the dose dumping. These are associated with problems like storage, leaching, aggregation. Extra care should be taken while manufacturing these carriers. Expensive. 24 International journal of pharmaceutics
  • 25. Vesicular drug delivery systems: Deliver the drug at a rate directed by need of body during the period of treatment, and channel the active entity to the site of action. Various routes of administration, to achieve targeted and controlled drug delivery . Improves the therapeutic efficacy and reduces the side effects. Targeting means the delivery of drugs to receptor, organs or any other specific part of body to which one wishes to deliver the entire drug . 25
  • 26. Deliver the drug at target site; these include immunoglobulins, serum proteins, synthetic polymers, microspheres, liposomes, niosomes, erythrocytes . Improve : Therapeutic index, solubility, stability and rapid degradation of drug molecules. 26 Continue… umar R, Kumar S, Jha SS, Jha AK. Vesicular system-carrier for drug delivery.
  • 27. Types: Lipoidal bio-carriers for site specific targeting 1. Liposomes 5. Sphingosomes 2. Emulsomes 6. Transferosomes 3. Enzymosomes 7. Pharmacosomes 4. Ethosomes 8. Virosomes Non- lipoidal biocarriers for site-specific targeting 1. Niosomes 3. Aquasomes 2. Bilosomes 27
  • 28. 1] Liposomes :  20 nanometers to several micrometers in size.  Lipid bilayer structures.  Enclosed by a membrane, composed of lipid molecules :both hydrophilic and lipophilic drugs can be successfully entrapped.; within bilayer membrane.  Hydrophilic drugs get entrapped in the central aqueous core of the vesicles.  Attach to cellular membrane :fuse with them, releasing their content into the cell.  Drug trapped inside is released. 28 Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.
  • 29. 2] Emulsomes :  Lipid based drug delivery system . parenteral delivery of drugs having poor aqueous solubility.  Internal core is made up of fats and triglycerides, stabilized : o/w emulsion , addition of high concentration of lecithin.  Characteristics of both liposomes and emulsions.  Solidified or semi solidified internal oily core : better opportunity to load lipophilic drugs in high concentration.  Enhanced drug delivery.  Improved preclinical efficacy for oral route. 29 Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.
  • 30. 3 ]Enzymosomes:  proteins like enzymes :delivered through several approaches. Like polymeric carriers; aqueous space of lipid and bilayered vesicles. But delivery by attachment on surface of liposomes has shown the prominent response for the development of antibodies at the target site.  Enzymes upon complexing with lipids : enzymosomes.  developed with long circulation time in the blood.  accumulate at inflammed target sites.  maintaining enzymatic activity in its intact form . 30
  • 31. Example :  Milk or dairy product  Use : digest-protein product 31
  • 32. 4] Ethosomes :  Developed for delivering the drugs having low penetration power through skin. Soft lipid vesicles : size range from tens of nanometers to microns.  containing phospholipids, alcohol : high concentration and water.  Better skin permeation ability.  Surface negative net charge to ethosomes due to which size of vesicles decreases.  Used for delivery of various antifungal agents, antiviral agents.  Pharmacological efficacy in drug targeting : transdermal and dermal sites for the treatment of various skin diseases. 32 Gangwar S, Singh S, Garg G. Ethosomes: a novel tool for drug delivery through skin
  • 34. 5] Sphingosomes  Introduced to overcome the stability problems of liposomes.  Presence of sphingolipids instead of phospholipids present in liposomes.  Used : liposomes are prone to undergo chemical Degradation. : oxidation and hydrolysis of ester linkage.  Targeting of the drug to the site of action, because of being biodegradable,  Targeting to tumour tissues: site-specific ligands to achieve active targeting.  Better drug retention.  Ability to benefit from this novel encapsulation. 34 Samad A, Sultana Y, Aqil M. Liposomal systems: an update review. Curr Drug Deliv.
  • 36. 6] Transferosomes :  Transferosome means carrying body.  Squeeze itself through a pore, smaller than its size owing to its elasticity,  Enhance the skin penetration and deliver the drug non- invasively through the skin barrier .  Used : as carrier, controlled and targeted delivery of proteins, peptides, hormones, oral delivery of peptides likeinsulin and interferons.  10 timeÊs higher concentration in tissues under skin.  Anti-ovulatory effect as compared to plain drug for oral administration. 36 Sivasankar M, Katyayani T. Liposomesthe future of formulations. Int J Res Pharm Chem
  • 38. 7] Pharmacosomes Pharmacosomes are novel vesicular drug delivery systems having unique advantages over other drug delivery systems . Provides maximum entrapment efficiency. The three main components for the preparation of pharmacosomes are : drug, solvent and lipid. Drug should contain active hydrogen atom , esterified with lipid and form amphiphilic complexes, which facilitate membrane transfer. 38 soft hybrid biocarriers of supramolecular construction for drug delivery.
  • 39. 8] Virosomes : Reconstituted viral envelopes . Lipid bilayer , inserted viral glycoproteins. Different enveloped viruses. Liposomes with influenza virus hemagglutinin (HA) and neuraminidase (NA) spikes on their surface. Retain the cell entry and membrane fusion.  Use : vaccination for the efficient induction of antibody responses against the virus they are derived from . 39 World Journal pharmacy and pharmaceutical science
  • 42. 1] Niosomes: Vesicles on hydration of mixture of cholesterol and a single alkyl chain nonionic and non-toxic surfactant. Number of non-ionic surfactants have been used to prepare vesicles. Eg :., polyglycerol alkyl ethers, glucosyldialkyl ethers, crown ethers,and a series of spans and tweens. Vesicles are termed as niosomes. 10-1000nm consisting of spherical, uni or multilamellar and polyhedral vesicles in aqueous media. 42 World Journal pharmacy and pharmaceutical science
  • 43. Example :  Use : Mackup base 43
  • 44. 2] Bilosomes :  Novel innovative drug delivery carriers : deoxycholic acid incorporated into the membrane of niosomes.  Bile salt stabilized vesicles are known as bilosomes.  Therapeutic efficacy of drugs : stability in gastro intestinal tract.  Increase the bioavailability of drugs .  Liver and release the drug, so found to be an effective tool in drug targeting to liver.  Found to stabilize : vesicles in GI environment. 44 . Formulation and characterization of vesicular drug delivery system for anti-HIV drug
  • 46. 3] Aquasomes  One of the most recently developed delivery system for bioactive molecules.  Aquasomes are three layered structures. (core, coating and drug)  Self-assembled through non covalent bonds, ionic bonds and vanderwaals forces.  Aquasomes are spherical 60- 300nm size particles .  Aquasomes can be used as red blood cell substitutes. : release of oxygen by haemoglobin. 46 Functionalized nanocarriers to image and target fungi infected cells.
  • 47. Example :  Used as vaccines for delivery of viral antigen, targeted intracellular gene therapy, for delivery of insulin and enzymes like DNAase and pigments/dyes . 47
  • 48. Summary:  Drug delivery research areas is continuously broaden and modified as a results of the realization of many factors (such as poor drug solubility and/or absorption, rapid metabolism, high fluctuation in the drug plasma level and variability) adversely affect in-vivo results, in conventional drug delivery system.  Lipids are one of the basic building blocks of biological membranes.  Nanoscale-based delivery strategies are beginning to make a significant impact on global pharmaceutical planning and marketing.  Among the approaches for exploiting nanotechnology developments in medicine, various nanoparticulates offer some unique advantages as pharmaceutical carriers in delivery systems and image enhancement agents.  The review illustrates the various classes of particulate lipid-based carriers among them; lipoproteins, lipid nanoparticles either; solid lipid nanoparticles, nanostructured lipid carriers, or lipid drug conjugates, lipid nanocapsules, and liposomes.  Lipid-based particulate carriers’ applications in various areas were also addressed. 48
  • 49. Refrence:  International Journal of pharmacy ; Review article by :Department of pharmaceutics, Pullareddy institute of pharmacy,Andhrapradesh,India  .World Journal pharmacy and pharmaceutical science ,Teegala Ram Reddy College of Pharmacy, Meerpet Hyderabad, Telangana- India.  .Bhadra D , Gupta G , Bhadra S, Umamaheshwari RB , Jain N . ,Multicomposite ultrathin capsules for sustained ocular delivery of ciprofloxacin hydrochloride, J Pharm Pharm Sci. 2004 ; 16: 7(2):241-51  .Manish G, Vimukta S. Targeted drug delivery system: a review. Res J Chem Sci. 2011; 1(2):135-138. 49
  • 50.  Kumar R, Kumar S, Jha SS, Jha AK. Vesicular system-carrier for drug delivery. Der Pharmacia Sinica. 2011; 2(4):192-202.  Anwekar H, Patel S, Singhai AK. Liposome-as drug carrier.Int J Pharm Life Sci. 2011; 2(7): 945-951.  Wagner A, Uhl KV. Liposome technology for industrial purposes.J Drug Deliv. 2011; 2011:1-9.  Sivasankar M, Katyayani T. Liposomesthe future of formulations. Int J Res Pharm Chem. 2011; 1(2):259-267.  Lehtinen J, Raki M, Bergstrom KA, Uutela P, Lehtinem K, Hiltunen A, Pikkarainen J, Liang H, Pitkanen S, Maatta AM, Ketola RA, Yliperttula M, Wirth T, Urtti A. Pre-targeting and direct immunotargeting of liposomal drug carriers to ovarian carcinoma. Plosone. 2012; 7(7):1-10.  Doijad RC, Bhambere DS, Manvi FV, Deshmukh NV. Formulation and characterization of vesicular drug delivery system for anti-HIV drug. J Global Pharm Technol. 2009; 1(1):94100 50
  • 51. 51