Development of SMEDDS using natural lipophile: application to beta-Artemether delivery.
The objective of the present investigation was to formulate self-microemulsifying drug delivery systems (SMEDDS) using a novel, indigenous natural lipophile (N-LCT) as an oily phase. SMEDDS based on N-LCT and commercially available modified oil (Capryol 90) were formulated and their application in improving the delivery of a lipophilic anti-malarial drug, beta-Artemether (BAM) was also evaluated. BAM-loaded SMEDDS were characterized with respect to mean globule size and in vitro drug release profile in comparison to the marketed formulation (Larither). Comparative in vivo anti-malarial performance of the developed SMEDDS was evaluated against the (Larither in Swiss male mice infected with lethal ANKA strain of Plasmodium berghei. The parameters studied were percent parasitemia, activity against time and animal survival period. Both the BAM-SMEDDS showed excellent self-microemulsification efficiency and released >98% of the drug in just 15 min whereas (Larither) showed only 46% drug release at the end of 1h. The mean globule size for optimized BAM-SMEDDS was <100 nm. The anti-malarial studies revealed that BAM-SMEDDS resulted in significant improvement in the anti-malarial activity (P<0.05) as compared to that of (Larither) and BAM solubilized in the oily phases and surfactant. The developed SMEDDS highlight safety for use and potential applications of indigenous natural lipophile in the development of novel colloidal drug carriers.
Mandawgade
Sagar D
SD
Department of Pharmaceutical Sciences and Technology, University Institute of Chemical Technology (UICT), Mumbai 400019, India.
Sharma
Shobhona
S
Pathak
Sulabha
S
Patravale
Vandana B
VB
D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use / Q000633:toxicity; D000077549:Artemether; D037621:Artemisinins / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use / Q000633:toxicity; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions; D007928:Lethal Dose 50; D008288:Malaria / Q000188:drug therapy / Q000382:microbiology; D008297:Male; D051379:Mice; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D010962:Plasmodium berghei / Q000187:drug effects; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry
D000962:Antimalarials; D037621:Artemisinins; D004337:Drug Carriers; D004655:Emulsions; D009821:Oils; D013501:Surface-Active Agents; D000077549:Artemether