Preparation, characterization and reduction of burst release of BSA from biodegradable PLGA microspheres

Rahman, Md. Mokhlesur and Ansary, Rezaul Haque and Mohamed, Farahidah and Awang, Mohamed and Yunus, Kamaruzzaman and Katas, Haliza (2014) Preparation, characterization and reduction of burst release of BSA from biodegradable PLGA microspheres. In: 1st International Conference of Industrial Pharmacy (ICIP 2014), 16th-17th Aug. 2014, Kuantan, Pahang.

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Abstract

BSA loaded hydroxyl terminated-PLGA and acid-terminated-PLGA microspheres have been prepared by a conventional water-in-oil-in-water (w/o/w) and a modified water-in-oil-in-oil-in-water (w/o/o/w) emulsion solvent evaporation method. In modified w/o/o/w emulsion technique, 100 µl of BSA solution (30 mg/ml) in 1% aqueous PVA (w/v) was emulsified with 50 mg of carboxyl terminated-PLGA in ethyl acetate (EA). This water/oil emulsion was then emulsified with 50 mg of hydroxyl terminated-PLGA in dichloromethane (DCM). The obtained w/o/o emulsion was further emulsified with 10 ml of 1% PVA. The resulting w/o/o/w emulsion was transferred into 50 ml of 0.5% PVA (w/v) aqueous solution and stirred for three hours to evaporate EA/DCM solvent mixture by vacuum evaporation at room temperature. After that the microspheres were separated by centrifugation and washed 3 times with 60 ml distilled water and freeze dried overnight. In conventional w/o/w method, BSA loaded hydroxyl terminated-PLGA and acid terminated-PLGA microspheres have been prepared separately as well. The particle size distribution was expressed as the volume median diameter (D 50%). BSA encapsulation efficiency and in vitro release were determined by a micro BCA method. Microspheres prepared with w/o/w and w/o/o/w emulsion technique exhibited high encapsulation efficiency except formulation F3. High initial burst release of BSA was observed in all formulations prepared by w/o/w emulsion technique. A significant reduction of initial burst release of BSA (Table 2) was observed when microspheres were prepared by modified w/o/o/w emulsion method. The optimized formulation (F4) of BSA loaded microspheres was nonporous, smooth-surfaced, and spherical shape (Fig. 2) under field-emission scanning electron microscope (FE-SEM) with a mean particle size of 3.95 µm and encapsulation efficiency of 98.46%. In contrast, microspheres prepared with w/o/w double emulsion technique were porous (Fig. 1) which might be a reason of high initial burst release of BSA. It can be concluded that microspheres prepared with hydroxyl terminated-PLGA and carboxyl terminated-PLGA by modified w/o/o/w method can be proposed as a potential delivery system of therapeutic proteins.

Item Type:	Conference or Workshop Item (UNSPECIFIED)
Additional Information:	5269/38154
Uncontrolled Keywords:	Poly(lactide-co-glycolide), microspheres, burst release, protein instability etc.
Subjects:	Q Science > QD Chemistry
Kulliyyahs/Centres/Divisions/Institutes (Can select more than one option. Press CONTROL button):	Kulliyyah of Pharmacy
Depositing User:	Dr Mohd Mokhlesur Rahman
Date Deposited:	10 Sep 2014 11:22
Last Modified:	11 Jun 2018 14:01
URI:	http://irep.iium.edu.my/id/eprint/38154

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