Retno Sari and Meta Dian Feriza and Amani Syarahil and Andang Miatmoko and Dwi Setyawan (2020) Characterization and in vitro release study of artesunateloaded microparticles prepared using crosslinked- chitosan and its derivatives. Tropical Journal of Pharmaceutical Research, 19 (6). pp. 1139-1146. ISSN 1596-9827

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Abstract

Purpose: To determine the effect of crosslinking on the physical characteristics, recovery, and release of artesunate-loaded chitosan and carboxymethyl chitosan microparticles. Methods: The artesunate microparticles were prepared by means of ionic gelation-spray drying methods involving the use of a crosslinking agent i.e. tripolyphosphate for chitosan and CaCl2 for carboxymethyl chitosan. The drug-polymer solution mixture was introduced into the crosslinker solution and stirred for two hours at 500 rpm prior to drying at a temperature of 100 ºC, a pressure of 2 mbar and a flow speed of 6.0 mL/min. The resulting microparticles were subsequently evaluated for their morphology, physical state, drug content and in vitro drug release. Results: The results showed that the type of chitosan and crosslinking affected particle shape, surface roughness, drug recovery, and drug release. The artesunate microparticles prepared with cross-linked polymer demonstrated a lower encapsulation efficiency due to the barriers presented by the crosslinking agents. The use of carboxymethyl chitosan increased the release rate of the artesunate from the microparticles by up to 1.2 times (16.78 mg/ml.min½), while chitosan decreased it 0.7 times (9.12 mg/ml.min½) compared to artesunate alone (13.54 mg/ml.min½). Conclusion: The use of crosslinking agents and chitosan type affects the physical characteristics of artesunate in addition to its release rate from microparticles.

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