Development and Evaluation of Chloroquine Phosphate Microparticles using Solid Lipid as a Delivery Carrier
Journal: Journal of Drug Discovery, Development and Delivery (Vol.2, No. 1)Publication Date: 2015-02-25
Authors : Ogbonna JDN; Nzekwe IT; Kenechukwu FC; Nwobi CS; Amah JI; Attama AA;
Page : 1-8
Keywords : Solid lipid microparticles; Chloroquine; Parasitemia; Haematological parameters; Histological studies;
Abstract
The aim of the study was to formulate and evaluate in vitro-in vivo Chloroquine (CQ)-loaded Solid Lipid Microparticles (SLMs). CQ-loaded SLMs were prepared by hot homogenization, lyophilized and characterized using particle size, pH stability, Loading Capacity (LC) and Encapsulation Efficiency (EE). In vitro release of CQ was performed in SIF and SGF and in vivo study done using Peter's Four day in mice, there after kidney and liver of the mice were subjected to histological studies. The formulations exhibited high entrapment efficiency and yield. Timedependent pH stability studies showed little variations with range from 3.93±0.21- 5, 46±0.23. The release profiles of CQ-loaded SLMs showed a gradual, steady release of the drug at various intervals in both SIF and SGF compared to the commercial CQ samples for 8 h. The in vivo study showed a high percentage reduction in parasitemia with minimal effect on vital organs. The SLMs exhibited sustained release with a pH-dependent release profile as the highest release was obtained in SIF than in SGF. The results showed that the percentage reduction in parasitemia of the optimized SLMs formulation (87.01%) had better activity than the commercial sample (84.12%). The histological studies revealed that the SLMs formulations have no harmful effects on the organs of the mice. SLMs formulations might be an alternative for delivery of CQ to patients with parasitemia.
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