Pharmacosomes: the lipid-based new drug delivery system.

HNB Garhwal University Srinagar, Department of Pharmaceutical Sciences, Garhwal-246174, India.
Expert Opinion on Drug Delivery (Impact Factor: 4.87). 07/2009; 6(6):599-612. DOI: 10.1517/17425240902967607
Source: PubMed

ABSTRACT Lipid-based drug delivery systems have been investigated in various studies and shown their potential in controlled and targeted drug delivery. Pharmacosomes are amphiphilic phospholipid complexes of drugs bearing active hydrogen that bind to phospholipids. Pharmacosomes impart better biopharmaceutical properties to the drug, resulting in improved bioavailability. Pharmacosomes have been prepared for various non-steroidal anti-inflammatory drugs, proteins, cardiovascular and antineoplastic drugs. Developing the pharmacosomes of the drugs has been found to improve the absorption and minimize the gastrointestinal toxicity. This article reviews the potential of pharmacosomes as a controlled and targeted drug delivery system and highlights the methods of preparation and characterization.

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    ABSTRACT: In th e p res en t study, ta m oxif en -p h os p h ol ip id co m p l ex ( TM X-P L C) wa s de vel o p ed an d e va lu ate d for its impact on s o lu bi li ty an d bi o avai la b il it y of ta m oxif en . TM X-P L C wa s p rep a red by s o lven t evap o rat io n m e th od and c ha racte r iz ed . FTIR reve al e d th e di sa p p ea ran ce of th e ch ara cte r is ti c pe ak s of TMX in th e c om p lex, wh i ch ca n be du e to wea ke n in g , rem oval or s h ie l di ng by th e phospholi pid m o le c ul e. Th i s p h en om e n on co u ld be du e to pa cki n g of TM X in th e hyd rop ho bi c cavi ty of p h os p h ol ip id an d be in g hel d by van de r Wa a l s fo rc es an d hyd ro ph o bi c in tera ct i on s . Th i s o bs er vati on wa s co n fi rme d by DSC and PX RD . TM X-P L C exh ib ite d in cr ea s ed so lu bi l it y, di s so l ut io n rate wi th de cre as ed di st r i bu ti o n co ef fi ci en t indicating it s in cr ea s ed hyd rop h il ic i ty. Ora l bi oavai l ab i li ty of TM X an d TMX-P LC were evalu ate d in Sp rag ue -D awl ey (SD) rat s . TM X- PL C exh i bi ted co ns i de rab l e en h an ce m e nt in th e bi oavai l ab i li ty wi th an i n cre as e in C max (0.85 vs. 0.40 m g/mL), t 1/2 (22.47 vs . 13.93 h), and AU C 0 –1(15.29 vs. 8.62 m g h/mL) with 212.25% relative bioavailability. This enhancement can be attributed to the improvement of the aqueous solubility of the complex and a probable decrease in its extent of intestinal and hepatic metabolism. Thus, phospholipid complexation holds a promising potential for increasing oral bioavailability of TMX.
    International Journal of Pharmaceutics 473 (2014) 1– 9. 10/2014;
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    ABSTRACT: Aim: The aim of the study is to improve the solubility and dissolution of furosemide (a potent high ceiling diuretic used for the treatment of hypertension and a class IV drug i.e. low solubility and low permeability drug as per the Biopharmaceutical Classification System) by preparing its phospholipid complexes or pharmacosomes. Materials and Methods: Furosemide was complexed with phosphatidylcholine in four different molar ratios (1:1, 1:2, 1:3 and 1:4) by conventional solvent evaporation technique. The pharmacosomes prepared were evaluated for drug content, solubility, X ray powder diffraction and in vitro dissolution study. Results: Pharmacosomes of furosemide showed high drug content ranging from 88.30 to 100 %. X ray powder diffraction studies confirmed the formation of phospholipid complex and the amorphization of drug in the complex. The water solubility was found to be increased up to six fold in the complexes. The octanol solubility also increased in the complexes indicating the probable increase in permeability. The in vitro dissolution profile of the prepared complexes was found to be much better than furosemide. Conclusion: It was concluded that the phospholipid complexes can be effectively used for improving the solubility, dissolution, permeability and hence the bioavailability of furosemide like class IV drugs.
    Drug Development and Therapeutics. 08/2014; 5(2):172-176.
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    International Journal of Pharmaceutics. 10/2014; 473(s 1–2):1–9.


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May 16, 2014