Effect of Formulation Variables on the Performance of Doxycycline-Loaded PLA Microsphere
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RESEARCH ARTICLE-CHEMICAL ENGINEERING
Effect of Formulation Variables on the Performance of Doxycycline-Loaded PLA Microsphere Shu Yen Cheng1 · John O. Akindoyo1 · Mariatti Jaafar1 · Zuratul Ain Abdul Hamid1 Received: 18 November 2019 / Accepted: 26 April 2020 © King Fahd University of Petroleum & Minerals 2020
Abstract Polymeric materials are currently being investigated as potential drug carriers. However, their performance is highly influenced by various factors especially the formulation variables. Herein, doxycycline-loaded PLA microspheres were prepared using the double emulsion solvent evaporation method and the effects of formulation variables were investigated. Specifically, particle size distribution, encapsulation efficiency and in vitro drug release behavior were evaluated for different formulations. In addition, antimicrobial activity of the doxycycline-loaded PLA microspheres was studied through the agar well diffusion method. Results showed that the addition of 4% NaCl into the external aqueous phase helped to improve the encapsulation efficiency, which subsequently influenced the drug release behavior of the microspheres. Specifically, about 66% of the doxycycline was encapsulated within PLA microspheres. Notably, slower drug release behavior was obtained by increasing the aqueous/organic phase volume ratio, polymer concentration and NaCl concentration in the external aqueous phase. However, increase in the particle size of microspheres resulted in lower encapsulation and antibacterial efficiencies. This study reveals that through proper manipulation of formulation variables, high-performance PLA microspheres suitable for use as carrier for various drugs can be prepared. Keywords Poly(lactic acid) · Doxycycline · Emulsification solvent evaporation · Formulation variable · Drug delivery
1 Introduction Drug delivery is a method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals [1]. Specifically, carrier-based drug delivery systems are currently being widely investigated based on the desirable features of this approach, and its suitability to minimize drug loss and other potential drug-related side effects [2, 3]. Notably, the drug carrier plays a vital role in transporting the active ingredients across the biological membranes to the desired site [4]. As such, careful selection of drug carriers is very important. Herein, biodegradable polymeric drug carriers are of particular interest. It is noteworthy that in this regard there are many potential drug carriers including polymer-based disk, rods, pellets and microparticles or microspheres. Particularly, there is an increasing
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Mariatti Jaafar [email protected] Department of Biomaterials Niche Groups, School of Materials and Mineral Resources Engineering, Engineering Campus, Universiti Sains Malaysia, 14300 Nibong Tebal, Pulau Pinang, Malaysia
interest in biodegradable microspheres which is directly associated with their salient properties for drug delivery. Specifically, they can be used t
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