Preparation and characterization of resiquimod-loaded microsponges
INTRODUCTION Microsponges are porous microspheres, which can be used as a polymeric delivery system to deliver active pharmaceutical ingredient such as resiquimod in a controlled release manner. The objectives of this study were to encapsulate and characterize resiquimod in the microsponges. M...
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| Format: | Conference or Workshop Item |
| Language: | English |
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2015
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| Online Access: | http://irep.iium.edu.my/45044/ http://irep.iium.edu.my/45044/1/45044.pdf |
| Summary: | INTRODUCTION
Microsponges are porous microspheres, which can be used as a polymeric delivery system to deliver active pharmaceutical ingredient such as resiquimod in a controlled release manner. The objectives of this study were to encapsulate and characterize resiquimod in the microsponges.
MATERIALS AND METHODS
100mg of ethylcellulose and 1mg of resiquimod was dissolved in dichlromethane (DCM) or ethylacetate (EA) and was poured into 1% of polyvinyl alcohol (PVA). The solvent was evaporated in a fume hood. Particle size of microsponges were determined by BT-9300H Laser Particle Size Analyzer. The microspheres were coated with gold palladium alloy and observed with a field emission scanning electron microscope FESEM at an intensity of 10kV.
RESULTS AND DISCUSSION
With 10 mL DCM with 20 mL PVA 1%, the entrapment efficiency (EE) of resiquimod is 31.32 ± 2.22. The amount of DCM used in the microsponge preparation decreased to 5 mL with 20 mL PVA 1% in which the %EE was found to be high (32.58 ± 1.76%). The preparation with 5 mL EA and 5 mL DCM with 20 mL PVA 1% resulted in lower % EE (23.75 ± 0.30). This might be due to the hardening time of microspheres is faster with EA compared to DCM. The microsponges prepared have homogeneous particle size ranging from 3.82 to 4.21 µm. The surface of microspheres prepared by EA are mainly appeared to be wrinkle, meanwhile microspheres prepared by DCM appeared to have smooth surfaces which indicates rapid polymer precipitation.
FigFig. 1. FESEM results of microsponges prepared using DCM in dispersion phase as A) 1 mL, B) 2.5 mL C) 5 mL D) 10 mL.
CONCLUSIONS
The type and amount of organic solvents play a vital role in the resulted microspheres. The highest % EE and optimum particle size was obtained with low amount of organic solvents.
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