Development and characterization of emulsomes for sustained and targeted delivery of an antiviral agent to liver

Author:

Vyas S P1,Subhedar Rasika1,Jain Sanyog2

Affiliation:

1. Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar (M.P.), India 470003

2. Division of Radiopharmaceuticals, Nano Tech and Stem Cell Research, Institute of Nuclear Medicine and Allied Sciences, Defence Research and Development Organization, Brig. S. K. Mazumdar Road, Timarpur, Delhi-110 054 India

Abstract

Abstract 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.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

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