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    Dissolution and physicochemical stability enhancement of artemisinin and mefloquine co-formulation via nano-confinement with mesoporous SBA-15

    Year: 2017

    Journal: Colloid Surf. B-Biointerfaces, Volume 155, JUL 1, page 560–568

    Authors: Letchmanan, Kumaran; Shen, Shou-Cang; Ng, Wai Kiong; Tan, Reginald B. H.

    Organizations: GlaxoSmithKline (GSK) [R-279-000-329592]; Science and Engineering Research Council of A*STAR (Agency for Science, Technology and Research), Singapore; National University of Singapore

    Keywords: Artemisinin-based combination therapy; Excipient; Supersaturation; Dissolution rate; Physicochemical stability

    The objective of this study is to enhance the dissolution rate, supersaturation and physicochemical stability of combination of two poorly water-soluble anti-malarial drugs, artemisinin (ART) and mefloquine (MFQ), by encapsulating them inside mesoporous silica (SBA-15) via co-spray drying. Characteristic studies such as powder X-ray diffraction (PXRD), transmission electron microscopy (TEM) and scanning electron microscope (SEM) clearly indicate the amorphization of the crystalline drugs. ART/MQF/SBA-15 formulations show a superior dissolution enhancement with a burst release of more than 95% of drugs within 30 min. In addition, the combination formulation exhibits a stable supersaturation enhancement by 2-fold higher than that of the untreated crystalline counterparts. ART/MQF/SBA-15 samples possess excellent physicochemical stability under 2 different moderate storage conditions for 6 months. The amorphization of ART and MFQvia nano-confinement using mesoporous SBA-15 is a potentially promising approach to enhance the solubility of poorly water-soluble anti-malarial drugs that co-formulated into a single dosage form. (C) 2017 Elsevier B.V. All rights reserved.
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