[논문]Development of New Reverse Micellar Microencapsulation Technique to Load Water-Soluble Drug into PLGA Microspheres

Kim Hyun Joo; Cho Mi Hyun; Sah Hong Kee

doi:10.1007/bf02977807

Development of New Reverse Micellar Microencapsulation Technique to Load Water-Soluble Drug into PLGA Microspheres 원문보기

Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, v.28 no.3, 2005년, pp.370 - 375

Kim Hyun Joo (Department of Pharmaceutical Sciences, College of Pharmacy, Catholic University of Daegu) , Cho Mi Hyun (Department of Pharmaceutical Sciences, College of Pharmacy, Catholic University of Daegu) , Sah Hong Kee (Department of Pharmaceutical Sciences, College of Pharmacy, Catholic University of Daegu)

Abstract ▼ AI-Helper

The objective of this study was to develop a new reverse micelle-based microencapsulation technique to load tetracycline hydrochloride into PLGA microspheres. To do so, a reverse micellar system was formulated to dissolve tetracycline hydrochloride and water in ethyl formate with the aid of cetyltrimethylammonium bromide. The resultant micellar solution was used to dissolve 0.3 to 0.75 g of PLGA, and microspheres were prepared following a modified solvent quenching technique. As a control experiment, the drug was encapsulated into PLGA microspheres via a conventional methylene chloride-based emulsion procedure. The microspheres were then characterized with regard to drug loading efficiency, their size distribution and morphology. The reverse micellar procedure led to the formation of free-flowing, spherical microspheres with the size mode of 88 ~m. When PLGA microspheres were prepared following the conventional methylene chloride-based procedure, most of tetracycline hydrochloride leached to the aqueous external phase: A maximal loading efficiency observed our experimental conditions was below $5\%$. Their surfaces had numerous pores, while their internal architecture was honey-combed. In sharp contrast, the new reverse micellar encapsulation technique permitted the attainment of a maximal loading efficiency of 63.19 $\pm$$0.64\%$. Also, the microspheres had smooth and pore-free surfaces, and hollow cavities were absent from their internal matrices. The results of this study demonstrated that PLGA microspheres could be successfully prepared following the new reverse micellar encapsulation technique.

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대상 데이터

PLGA with a lactide:glyc이ide ratio of 75:25 (hiherent viscosity = 0.69 dUg in CHCI3 at 30℃, lot number D01066) was purchased from Birmingham Polymers, Inc. (Birmingham, AL, USA). The polymer was abbreviated as PLGA75:25 in the text.

이론/모형

The size distribution of microspheres was measured by laser diffraction analysis using a unified scatter technique (Microtrac X100 particle size analyzer; Microtrac, Inc., Montgomeryville, PA, USA). Aliquots of microsphere samples were dispersed in water by gentle stirring, which was loaded into the particle size analyzer.

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DOI : 10.1007/BF02977807 [무료]
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