- 作者: Lakshmi N Ramana; Swaminathan Sethuraman; Udaykumar Ranga; Uma M Krishnan
- 作者服務機構: Centre for Nanotechnology & Advanced Biomaterials (CeNTAB), School of Chemical & Biotechnology, SASTRA University, India
- 中文摘要: --
- 英文摘要:
Background
The treatment of AIDS remains a serious challenge owing to high genetic variation of
Human Immunodeficiency Virus type 1 (HIV-1). The use of different antiretroviral
drugs (ARV) is significantly limited by severe side–effects that further compromise the
quality of life of the AIDS patient. In the present study, we have evaluated a liposome
system for the delivery of nevirapine, a hydrophobic non-nucleoside reverse transcriptase
inhibitor. Liposomes were prepared from egg phospholipids using thin film hydration.
The parameters of the process were optimized to obtain spherical liposomes below 200
nm with a narrow polydispersity. The encapsulation efficiency of the liposomes was
optimized at different ratios of egg phospholipid to cholesterol as well as drug to total
lipid. The data demonstrate that encapsulation efficiency of 78.14% and 76.25% were
obtained at egg phospholipid to cholesterol ratio of 9:1 and drug to lipid ratio of 1:5,
respectively. We further observed that the size of the liposomes and the encapsulation
efficiency of the drug increased concomitantly with the increasing ratio of drug and lipid
and that maximum stability was observed at the physiological pH. Thermal analysis of
the drug encapsulated liposomes indicated the formation of a homogenous drug–lipid
system. The magnitude of drug release from the liposomes was examined under different
experimental conditions including in phosphate buffered saline (PBS), Dulbecco’s
Modified Eagle’s Medium (DMEM) supplemented with 10% fetal bovine serum or in the
presence of an external stimulus such as low frequency ultrasound. Within the first 20
minutes 40, 60 and 100% of the drug was released when placed in PBS, DMEM or when
ultrasound was applied, respectively. We propose that nevirapine–loaded liposomal formulations reported here could improve targeted delivery of the anti-retroviral drugs to
select compartments and cells and alleviate systemic toxic side effects as a consequence. - 中文關鍵字: --
- 英文關鍵字: --