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Liposomal drug delivery - an emerging trend for the treatment of tuberculosis

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Neha Rai *, Richa Tripathy , Vikas Soni . Department of pharmaceutical sciences,Dr.H.S.Gour Central University Sagar (M.P.) INTRODUCTION Liposomes are nano size artificial vesicles of spherical shape that can be produced from natural phospholipids and cholesterol. Bangham discovered that phospholipids combined with water immediately forms a bi-layered sphere, because one end of each molecule is water soluble, while the opposite end is water insoluble. Liposome based drug delivery system, offer the potential to enhance therapeutic index of anti-cancer agents, either by increasing the drug concentration in tumor cells and/or by decreasing the exposure in normal tissue exploiting enhanced permeability and retention effect phenomenon and by utilizing targeting strategies. CONCLUSION : Formulations Active ingredients Applications of liposomes formulations Biological activity % entrapment efficiency Route of administration Quercetin liposomes Qurecetin Reduced dose,enhance penetration in BBB Antioxidant Anticancer 60% Intranasal Liposomes encapsulated silymarin Silymarin Improve bioavailability Hepatoprotective 69.22± 0.6% Buccal Curcumin liposome curcumin Long circulating Anticancer 88.27± 2.16% In vitro Flavonoids liposomes Quercetin and rutin Bleeding of flavonoids with Hb is enhanced Hemoglobin - In vitro Garlicin liposome Garlicin Increase efficiency Lungs 90.77% - Catechins liposome Catechins Increased permiation through skin Antioxidant & chemopreservative 93.0± 0.1% Transdermal Colchicine liposome Colchicine Enhance skin accumulation, prol- -ong drug release Antigout 66.3± 2.2% Topical LIPOSOMAL DRUG DELIVERY IN T.B. TREATMENT LIPOSOMAL HERBAL FORMULATIONS Despite being an ancient disease, TB continues to be a major health concern around the world. Pulmonary TB is the most common manifestation of TB and the development of controlled release formulations of anti-TB drugs that are either inhaled or intravenously administrated and directly delivered to the lungs seems a possible approach in the development of novel and more efficient therapeutic alternatives. Liposomes are nanobiotechnological systems with great potential to be applied in drug delivery for the treatment of TB. Their use increases the therapeutic index of anti-TB drugs, and they are safe and biocompatible. Various properties of these carriers, including size, surface charge, composition and the presence of ligands, significantly alter the specificity to alveolar macrophages. Therefore, liposomes represent appealing nanocarrier systems for anti-TB drugs and possess large potential for the treatment of pulmonary TB. REFERENCES METHOD OF LIPOSOME PREPARATION BIOAVAILABILITY OF LIPOSOMES Silymarin is poorly absorbed (20-50%) from the gastrointestinal tract but incorporation of silymarin into liposomal dosage form administered buccally can improve its bioavailability. The introduced hybrid liposomal silymarin formula for buccal administration have the advantage of exerting a mucoadhesive effect . LIPOSOME FOR DRUG DELIVERY 1) Blumenthal M, Goldberg A, Brinkmann J. Herbal medicine. Integrative Medicine Communications. Newton; 2000. 2) Xiao YL, Li B. Chine Trad Herb Drugs 2002;33:385. There are several methods:- 1) Multi - laminar vesicles: • a) Liquid hydration method • b) Solvent spherule method 2) Unilaminar vesicles: • a) Freeze-Thaw method • b) Micro fluidization method • c) Reverse phase evaporation method • d) Sanitation method 1) Liposome can carry both the hydrophobic and hydrophilic drug, therefore, liposome as a drug carrier can indiscriminately deliver drugs through the cell membrane. 2) Liposome herbal therapy acts as a carrier for small cytotoxic molecules and as vehicle for macromolecules as gene. 3) Liposome formulation can produce sustained and controlled release of formulation and enhances drug solubility. 4) Standardized plant extracts or mainly polar phytoconstituents like flavonoids,terpenoids,tannins when administered through liposomes show much better bioavailability. INDUSTRIAL METHOD 1) Detergent dialysis method 2) Microlludisation method 3) Preliposomes 4) Freeze drying method Drug crystallized in aqueous fluid Lipid bilayer Lipid soluble drug in bilayer DNA
Transcript

Neha Rai*, Richa Tripathy, Vikas Soni.

Department of pharmaceutical sciences,Dr.H.S.Gour Central University Sagar (M.P.)

INTRODUCTION

Liposomes are nano size artificial vesicles of spherical shape that can be produced

from natural phospholipids and cholesterol. Bangham discovered that phospholipids

combined with water immediately forms a bi-layered sphere, because one end of each

molecule is water soluble, while the opposite end is water insoluble.

Liposome based drug delivery system, offer the potential to

enhance therapeutic index of anti-cancer agents, either by

increasing the drug concentration in tumor cells and/or by

decreasing the exposure in normal tissue exploiting

enhanced permeability and retention effect phenomenon

and by utilizing targeting strategies.

CONCLUSION :

Formulations Active

ingredients

Applications of

liposomes

formulations

Biological activity %

entrapment

efficiency

Route of

administration

Quercetin

liposomes

Qurecetin Reduced

dose,enhance

penetration in BBB

Antioxidant

Anticancer

60% Intranasal

Liposomes

encapsulated

silymarin

Silymarin Improve

bioavailability

Hepatoprotective 69.22±

0.6%

Buccal

Curcumin liposome curcumin Long circulating Anticancer 88.27±

2.16%

In vitro

Flavonoids

liposomes

Quercetin

and rutin

Bleeding of

flavonoids with Hb

is enhanced

Hemoglobin - In vitro

Garlicin liposome Garlicin Increase efficiency Lungs 90.77% -

Catechins liposome Catechins Increased

permiation through

skin

Antioxidant &

chemopreservative

93.0±

0.1%

Transdermal

Colchicine

liposome

Colchicine Enhance skin

accumulation, prol-

-ong drug release

Antigout 66.3±

2.2%

Topical

LIPOSOMAL DRUG DELIVERY IN T.B. TREATMENT

LIPOSOMAL HERBAL FORMULATIONSDespite being an ancient disease, TB continues to be a major health

concern around the world. Pulmonary TB is the most common

manifestation of TB and the development of controlled release

formulations of anti-TB drugs that are either inhaled or intravenously

administrated and directly delivered to the lungs seems a possible

approach in the development of novel and more efficient therapeutic

alternatives. Liposomes are nanobiotechnological systems with great

potential to be applied in drug delivery for the treatment of TB. Their

use increases the therapeutic index of anti-TB drugs, and they are safe

and biocompatible. Various properties of these carriers, including size,

surface charge, composition and the presence of ligands, significantly

alter the specificity to alveolar macrophages. Therefore, liposomes

represent appealing nanocarrier systems for anti-TB drugs and possess

large potential for the treatment of pulmonary TB.

REFERENCES

METHOD OF LIPOSOME PREPARATION

BIOAVAILABILITY OF LIPOSOMES

Silymarin is poorly absorbed (20-50%) from the gastrointestinal tract but incorporation of

silymarin into liposomal dosage form administered buccally can improve its

bioavailability. The introduced hybrid liposomal silymarin formula for buccal

administration have the advantage of exerting a mucoadhesive effect .

LIPOSOME FOR DRUG

DELIVERY

1) Blumenthal M, Goldberg A, Brinkmann J. Herbal medicine. Integrative Medicine Communications. Newton; 2000. 2) Xiao YL, Li B. Chine Trad Herb Drugs 2002;33:385.

There are several methods:-

• 1) Multi-laminar vesicles:

• a) Liquid hydration method

• b) Solvent spherule method

• 2) Unilaminar vesicles:

• a) Freeze-Thaw method

• b) Micro fluidization method

• c) Reverse phase evaporation method

• d) Sanitation method

1) Liposome can carry both the hydrophobic and hydrophilic drug,

therefore, liposome as a drug carrier can indiscriminately

deliver drugs through the cell membrane.

2) Liposome herbal therapy acts as a carrier for small cytotoxic

molecules and as vehicle for macromolecules as gene.

3) Liposome formulation can produce sustained and controlled

release of formulation and enhances drug solubility.

4) Standardized plant extracts or mainly polar phytoconstituents

like flavonoids,terpenoids,tannins when administered through

liposomes show much better bioavailability.

INDUSTRIAL

METHOD

1) Detergent dialysis method

2) Microlludisation method

3) Preliposomes

4) Freeze drying method

Drug crystallized in aqueous fluid

Lipid bilayer

Lipid soluble drug in bilayer

DNA

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