Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Characterization and in vitro release study of artesunate-loaded microparticles prepared using crosslinked-chitosan and its derivatives

Retno Sari , Meta Dian Feriza, Amani Syarahil, Andang Miatmoko, Dwi Setyawan

Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Campus C UNAIR, Mulyorejo, Surabaya 60115, Indonesia;

For correspondence:- Retno Sari Email: retno-s@ff.unair.ac.id

Accepted: 23 May 2020 Published: 30 June 2020

Citation: Sari R, Feriza MD, Syarahil A, Miatmoko A, Setyawan D. Characterization and in vitro release study of artesunate-loaded microparticles prepared using crosslinked-chitosan and its derivatives. Trop J Pharm Res 2020; 19(6):1139-1146 doi: 10.4314/tjpr.v19i6.3

© 2020 The authors.
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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.

Keywords: Artesunate, Chitosan, Carboxymethyl chitosan, Crosslinking, Microparticle, Drug release