Development and characterization of emulsomes for sustained and targeted delivery of an antiviral agent to liver.
In this study we developed emulsomes, a novel lipoidal vesicular system with an internal solid fat core surrounded by a phospholipid bilayer. Plain emulsomal formulations composed of solid lipid (trilaurin or tristearin), cholesterol and soya phosphatidylcholine and stearylamine containing cationic emulsomes loaded with an antiviral drug (zidovudine) were prepared by a simple cast film method followed by sonication to produce emulsomes of nanometric size range. All different types of formulations were optimized for lipid ratios and characterized in-vitro for shape, morphology, size and in-vitro drug release profile. Emulsomal formulations displayed a sufficiently slow drug release profile (12-15% after 24 h). In-vivo organ distribution studies in rats demonstrated better uptake of emulsomal formulations by the liver cells. Further, a significantly higher (P < 0.05) liver concentration of drug was estimated over a period of 24 h for cationic emulsomes than for plain neutral emulsomes. We concluded that cationic emulsomes could fuse with the endosomal membrane due to charge-charge interaction and were released in the cytoplasm before lysosomal degradation and could sustain drug release over a prolonged period. The proposed cationic emulsome-based system showed excellent potential for intracellular hepatic targeting and the strategy could play a vital role in the effective treatment of life-threatening viral infections, such as hepatitis, HIV and Epstein-Barr virus infection.
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar (M.P.), India 470003.
S P
SP
Vyas
Rasika
R
Subhedar
Sanyog
S
Jain
D000588:Amines / Q000737:chemistry; D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002784:Cholesterol / Q000737:chemistry; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005260:Female; D008099:Liver / Q000378:metabolism*; D008297:Male; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D010713:Phosphatidylcholines / Q000737:chemistry; D051381:Rats; D012995:Solubility; D013678:Technology, Pharmaceutical; D014018:Tissue Distribution; D014280:Triglycerides / Q000737:chemistry; D015215:Zidovudine / Q000008:administration & dosage* / Q000493:pharmacokinetics
D000588:Amines; D019380:Anti-HIV Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D010713:Phosphatidylcholines; D014280:Triglycerides; D015215:Zidovudine; C004565:trilaurin; D002784:Cholesterol; C009317:stearylamine; C022618:tristearin