Development, characterization and antimalarial efficacy of dihydroartemisinin loaded solid lipid nanoparticles

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• 作者：Wesley N. Omwoyo ; PhD^a ; ^b ; Paula Melariri ; PhD^c ; Jeremiah W. Gathirwa ; PhD^d ; ^e ; ^{jgathirwa@kemri.org" class="auth_mail" title="E-mail the corresponding author} ; Florence Oloo ; PhD^e ; ^f ; Geoffrey M. Mahanga ; PhD^b ; Lonji Kalombo ; MEng^c ; Bernhards Ogutu ; PhD^d ; ^e ; Hulda Swai ; PhD^c
• 关键词：Dihydroartemisinin ; Solid lipid nanoparticles ; Nanomedicine drug delivery
• 刊名：Nanomedicine: Nanotechnology, Biology and Medicine
• 出版年：2016
• 出版时间：April 2016
• 年：2016
• 卷：12
• 期：3
• 页码：801-809
• 全文大小：454 K

文摘

Effective use of dihydroartemisinin (DHA) is limited by poor water-solubility, poor pharmacokinetic profile and unsatisfactory clinical outcome especially in monotherapy. To reduce such limitations, we reformulated DHA into solid lipid nanoparticles (SLNs) as a nanomedicine drug delivery system. DHA-SLNs were characterized for physical parameters and evaluated for in vitro and in vivo antimalarial efficacy. DHA-SLNs showed desirable particle characteristics including particle size (240.7 nm), particle surface charge (+ 17.0 mV), drug loadings (13.9 wt %), encapsulation efficacy (62.3%), polydispersity index (0.16) and a spherical appearance. Storage stability up to 90 days and sustained release of drug over 20 h was achieved. Enhanced in vitro (IC₅₀ 0.25 ng/ml) and in vivo (97.24% chemosuppression at 2 mg/kg/day) antimalarial activity was observed. Enhancement in efficacy was 24% when compared to free DHA. These encouraging results show potential of using the described formulation for DHA drug delivery for clinical application.

From the Clinical Editor

Malaria still poses a significant problem worldwide. One of the current drugs, artemisinin has been shown to be effective, but has poor water-solubility. The authors here described their formulation of making dihydroartemisinin (DHA) into solid lipid nanoparticles, with subsequent enhancement in efficacy. These results would have massive potential in the clinical setting.