This document discusses vesicular drug delivery systems (VDDS), including their classification, advantages, and formulation methods. It summarizes that VDDS can be classified as lipoidal or non-lipoidal carriers, with liposomal systems like liposomes, ethosomes, transfersomes discussed in detail. The advantages of VDDS include effective drug permeation, prolonged circulation time, reduced toxicity and cost of therapy. However, VDDS also have disadvantages like low drug loading efficiency and stability issues. The document provides an overview of various vesicular carrier preparation techniques for developing novel drug delivery systems.

1. SUMEL ASHIQUE
DEPT.PHARMACEUTICS
GURU NANAK INSTITUTE OF
PHARMACEUTICAL SCIENCE &
TECHNOLOGY

2.  Introduction
Classification of vesicular drug delivery system
 Lipoidal biocarrier
 Nonlipoidal biocarrier
 Advantages & Disadvantages
 Conclusion
 References

3. A novel drug delivery system is that delivers drug at
predetermined rate decided as per the requirement,
pharmacological aspects, drug profile, physiological conditions
of body etc. A Vesicular drug delivery system (VDDS) is the
system in which encapsulation of active moieties in vesicular
structure, which bridges gap between ideal and available of
novel drug delivery system.Various types of vesicular drug
delivery system like liposome, niosome, aquasome,
transferosome etc. were developed.

4. I. Effective permeation of drugs into cells
II. Prolongation of existence of drugs in systemic circulation.
III. As selective uptake is taken place so reduces toxicity.
IV. Reduces the cost of therapy.
V. Improves bioavailability.
VI. Hydrophilic-Lipophilic drugs can be incorporated.
VII. Sustained-release system function.
VIII.Delayed elimination of rapidly metabolized drugs.
IX. Overcomes the problems of the drug insolubility, instability,
and rapid degradations.

5. Along with numbers of advantages VDDS has some serious
disadvantages which restrict their use. Drugs passively , which
may lead to low drug loading efficiency and drug leakage in
preparation, preservation and transport in vivo. Need of
intensive sonication, lead to leakages of drug during storage.
Thus the major problem of their stability acts as a barrier and
thus limiting their use.

6. LIPOIDAL BIO –CARRIERS : Non-lipoidal biocarriers
 Liposomes Niosomes
 Ethosomes Bilosomes
 Transferosomes Aquasomes
 Sphingosomes
 Pharmacosomes
 Virosomes
 Phytosomes

7. Phospholipid+ cholesterol= Liposome.
 Classification Based on structure :
1. MLV (Multilamillar vesicles 0) (>0.5μm)
2. OLV(Oligolamillar vesicles )(0.1 to 10 μm)
3. ULV (Unilamillar vesicles) (All in size)
4. Multivesicular vesicles (>1.0μm)
 Classification based on Method of Preparation:
1. Mechanical dispersion
2. Solvent dispersion
1) Detergent removal

8. 1.Thin film hydration method.
2 Ultra sonication.
3.French Pressure cell.
4.Freeze thawed.
SOLVENT DISPERSION
1.Solvent injection method.
a) Ether injection.
b) Ethanol injection.
2.Reverse phase evaporation technique.

9. 1) Detergent removal.
a) Dialysis.
b) Column chromatography.
c) Dilution.
FREEZE THAW:
Phospholipid dissolved in t-butanol Freeze dride
liposome Add water
or saline
REVERSE PHASE EVAPORATION :
Lipid in water + aq. phase sonicate o/w emulsion

10. Organic solution evaporation gel formation vortex
liposome
ETHER INJECTION
Mixing of organic phase into aq. Phase
DIALYSIS
Detergents are removed from micelle by dialysis by lowering the
concentration of detergent in bulk aq. Phase.

11. FILM HYDRATION METHOD
Phospholipid + cholesterol
Organic solvent in RBF
Rotate clockwise to form
Film.
Now add PBS solution in which drug is dissolved.
now rotate anti-clockwise to entrapped the drug in film.
Liposomal solution.

12. MEMBRANE EXTRUSION METHOD
Fig; Liposomes Preparations using extractions techniques
based on polycarbonate filters

13. Phospholipid + Phyto constituents (2:1)
METHODS:
 Solvent evaporation
 Anti solvent pre-cipitation method.
 Salting out method
 Lyophilization method
 SOLVENT EVAPORATION METHOD
 A quantity of drug + polymer+ phospholipids taken in a
spherical bottom flask reflux with specific solvent at a temp
of (55℃-60℃). The mixture is concentrated to 5-10 ml to
get ppt which can be filtered & c0llected. Dride phytosome.

14. Phyto constituent + phospholipid dissolved in aprotic solvent(
acetone) complex formation isolated by precipitation.
LYOPHILIZATION METHOD:
Phospholipid + phyto constituent dissolved in different
solvent stirring till complex formation takes place.
Application:
Silybin-Nutraceuticals,antioxidant for liver.
Olive oil phytosome-antioxidant,anti inflammatory
Green tea phytosome-Anti carcinogenic
Grape seed phytosome- Antioxidant
Ginseng phytosome-Immunomodulator.

15. Non ionic surfactant vesicle obtained by hydrating
mixture of cholesterol + non-ionic surfactant.
METHODS:
Ether injection method:
Slowly introducing a solution of surfactant dissolved in di ethyl
ether into the warm water at 60℃ surfactant mixture
in ether is injected through 14 gauze needle. Vaporization of
ether leads to formation of single layered vesicles.
Sonication Method : In this method an aliquot of drug solution
in buffer is added to the surfactant cholesterol mixture
Mixture is probe sonicated at 60℃ for 3 mins using a sonicator
with a titanium probe to yield niosome.

16. Using RBF with 3 necks & positioned in a water bath to control
the temperature.
Water cooled reflux & thermometer is placed in 1st & 2nd position
& N2 through 3rd one.
Cholesterol+ surfactant are dispersed together in buffer solution
containing drug.
Dispersion mixed for 15 sec with shear homogenizer &
immediately bubbled at 70℃ using N2 to yield niosome.

17. As drug carriers: Carriers for Iobitridol a diagnostic agent used
for x-ray imaging.Topical niosomes may searve as local depot for
sustained release of dermally active compounds.
Delivery of peptide : through niosome ADH delivery increased
stability.
Carrier for Hb: Niosome permeable to O2 so Hb can be carried.
PHARMACOSOMES
Pharmacosomes are amphiphilic lipid vesicular system possessing
phospholipid complexes of drugs. Pharmacon means drugs &
Soma means Carrier thus Pharmacosomes means drug carriers.
System formed by linking drugs’ o the carrier. Colloidal dispersion
of drugs co-valant bond to lipids. Composed of Amphiphilic
prodrugs, so high drug loading amount & very low drug leakages
can be achieved easily.

18. 1. Hand shaking method
2. Ether injection method.
TRANSFEROSOMES
Transferosomes was introduced for the effective transdermal
delivery of number of low and high molecular weight drugs.
Transfersomes can penetrate the intact stratum corneum
spontaneously along two routes in the intracellular lipid that
differ in their bilayers properties. It consist of both hydrophilic
and hydrophobic properties, high deformability gives better
penetration of intact vesicles. Flexibility of transfersomes
membrane is achieved by mixing suitable surface-active
components in the proper ratios.

19. I. Transferosomes are chemically unstable because of their
predisposition to oxidative degradation.
II. Transferosomes formulations are expensive.
ETHOSOME:
Ethosomes are lipid based elastic vesicles. Phospholipids,
alcohol (In high concentration) & water. Size: Nanometers-
Microns. High concentration ethanol (20-50%).Lipid membrane
packed less tightly than conventional vesicles hence improved
drug distribution through stratum corneum. Increase fluidity of
cell membrane, increases cell permeability, lters solubility
properties of stratum corneum & Increase solubility of drugs, e.g.
Levonorgesterol, hydrocortisone, 5-flurouracil(TDDS).

20. Sphingosomes can be defined as colloidal, concentric bilayered
vesicles where aqueous compartment is entirely enclosed by a
bilayer membrane,mainly composed of natural or synthetic
sphingolipids.
Sphingosomes is more stable than the phospholipid
liposome because of the:
 Sphingolipid are built up by only amide and ether
linkage.
 They also contain a smaller amount of double bonds
then lecithin.
 They also absorb a smaller amount oil then lecithin that
in consequence change in geometry and diameter.

21. Advantages of Sphingosomes:
 Sphingosomes have better drug retention characteristics.
 They can be administered by subcutaneous, intravenous,
intra-arterial, intramuscular, oral, and transdermal routes of
drug administration and so forth.
 They provide selective passive targeting to tumor tissue.
 Sphingosomes increase efficacy and therapeutic index of the
encapsulated drug.
 Stability is increased via encapsulation.

22.  sphingolipids are expensive, sphingosomes are not
economic.
 Sphingosomes have poor entrapment efficiency.
 Method of Preparation of Sphingosome:
 Lipid Hydration Method
 Solvent Spherule Method.
 Sonication Method
 French Pressure Cell Method
 Solvent Injection Methods.
 Detergent Removal Methods
 Reverse Phase Evaporation Method.

23. Virosomes are spherical, unilamillar phospholipid bilayer
vesicles incorporating virus derived proteins to allow the
virosomes to fuse with the target cell.
They are lipid based , synthetic vesicles consisting of viral
surface glycoproteins.
They have a typical mean diameter in range 120-180 nm.
The envelop made up of influenza lipids constitute the
membrane and proteins called haemagglutinin (HA) and
neuraminidase (NA) are intercalated on it. The nucleocapsid and
the genetic material of the source virus is present inside the
envelop.

24. Because of the site specific targeting of drugs and lots of other
advantages, vesicular drug delivery system is gaining popularity
in
present scenario. Drugs can be directly targeted to their site of
action to prevent toxic and undesired effects to other sites,
further
these can be used for bioavailability enhancement of the drugs,
having poor bioavailability, to reduce the dose of drug
administered
and to enhance pharmacological action of drug. Vesicular
system
is valuable for drugs having narrow therapeutic index because
targeting of drug to their site of action improves the overall.

25. VESICULAR DRUG DELIVERY SYSTEMS: A NOVEL APPROACH
FOR DRUG TARGETING, SUNIL KAMBOJ, VIPIN SAINI1,
NANCY MAGON1, SUMAN BAL, VIKAS JHAWAT.
VESICULAR DRUG DELIVERY SYSTEM: A NOVEL APPROACH
KALPESH CHHOTALAL ASHARA, JALPA S. PAUN, M.M
SONIWALA, J.R.CHAVD, S. V. NATHAWANI, NITIN M. MORI
AND VISHAL P. MENDAPARA.
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