Development of SMEDDS using natural lipophile: Application to β-Artemether delivery
Abstract
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.
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Long-chain-triglyceride-based self-microemulsifying systems containing β-artemether were demonstrated to be safe and have a notable improvement in antimalarial activity in vivo compared with Larither.
“Long-chain-triglyceride-based self-microemulsifying systems containing β -artemether were demonstrated to be safe and have a notable improvement in the antimalarial activity in vivo compared with Larither.”
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- Authors
- Mandawgade, S. D., Sharma, S., Pathak, S., & Patravale, V. B.
- Affiliations
- Institute of Chemical Technology (IN)
- Tata Institute of Fundamental Research (IN)
- Corresponding author
- Patravale, Vandana B.
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2008-10
- Volume
- 362
- Issue
- 1-2
- Pages
- 179-183
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2059052125
- Cited by
- 100
- References
- 23
- Citations by year
- 2026: 1 · 2025: 4 · 2024: 5 · 2023: 5 · 2022: 6 · 2021: 5 · 2020: 10 · 2019: 4 · 2018: 3 · 2017: 7 · 2016: 8 · 2015: 7 · 2014: 8 · 2013: 9 · 2012: 10
- FWCI
- 1.87
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Directorate for Biological Sciences
- Institute of Psychology, Chinese Academy of Sciences
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- self-microemulsifying drug delivery system, Capryol 90, Plasmodium berghei, larval stages, globule size, in vitro drug release, colloidal drug carriers
- MeSH terms
- Artemether, Administration, Oral, Animals, Antimalarials, Biological Availability, Chromatography, High Pressure Liquid, Drug Carriers, Emulsions, Lethal Dose 50, Malaria, Male, Oils, Particle Size, Plasmodium berghei, Solubility, Surface-Active Agents, Drug Delivery Systems, Artemisinins, Mice
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