Optimization of entrapment efficiency and release of clindamycin in microsponge based gel
Abstract The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conv...
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2021
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oai:doaj.org-article:75666214f3064538b3f954124ee4207e2021-12-05T12:16:09ZOptimization of entrapment efficiency and release of clindamycin in microsponge based gel10.1038/s41598-021-02826-72045-2322https://doaj.org/article/75666214f3064538b3f954124ee4207e2021-12-01T00:00:00Zhttps://doi.org/10.1038/s41598-021-02826-7https://doaj.org/toc/2045-2322Abstract The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conversion of the hydrochloride salt to free base was done. By using an emulsion solvent diffusion method, we made six different formulations of microsponges containing CLN-free base by changing the proportions of polymer, emulsifier and the pH of the external phase. These formulations were studied for physical characterization and for drug- polymer interactions. The physical characterization showed that microsponge formulations coded by C5, C6 resulted in a better loading efficiency and production yield and their particle size was less than 30 µm. Scanning electron microscopy images showed the microsponges porous and spherical. C5, C6 microsponge formulation was prepared as gel in Carbopol and in vitro evaluated. The microsponge formulation gel C8 was found to be optimized. C8 released 90.38% of drug over 12 h and showed viscosity 20,157 ± 38 cp, pH of 6.3 ± 0.09 and drug content of 99.64 ± 0.04%. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed no significant interactions between excipients and drug.ALAA KHATTABAbdulhakim NattoufNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 11, Iss 1, Pp 1-10 (2021) |
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Medicine R Science Q ALAA KHATTAB Abdulhakim Nattouf Optimization of entrapment efficiency and release of clindamycin in microsponge based gel |
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Abstract The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conversion of the hydrochloride salt to free base was done. By using an emulsion solvent diffusion method, we made six different formulations of microsponges containing CLN-free base by changing the proportions of polymer, emulsifier and the pH of the external phase. These formulations were studied for physical characterization and for drug- polymer interactions. The physical characterization showed that microsponge formulations coded by C5, C6 resulted in a better loading efficiency and production yield and their particle size was less than 30 µm. Scanning electron microscopy images showed the microsponges porous and spherical. C5, C6 microsponge formulation was prepared as gel in Carbopol and in vitro evaluated. The microsponge formulation gel C8 was found to be optimized. C8 released 90.38% of drug over 12 h and showed viscosity 20,157 ± 38 cp, pH of 6.3 ± 0.09 and drug content of 99.64 ± 0.04%. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed no significant interactions between excipients and drug. |
format |
article |
author |
ALAA KHATTAB Abdulhakim Nattouf |
author_facet |
ALAA KHATTAB Abdulhakim Nattouf |
author_sort |
ALAA KHATTAB |
title |
Optimization of entrapment efficiency and release of clindamycin in microsponge based gel |
title_short |
Optimization of entrapment efficiency and release of clindamycin in microsponge based gel |
title_full |
Optimization of entrapment efficiency and release of clindamycin in microsponge based gel |
title_fullStr |
Optimization of entrapment efficiency and release of clindamycin in microsponge based gel |
title_full_unstemmed |
Optimization of entrapment efficiency and release of clindamycin in microsponge based gel |
title_sort |
optimization of entrapment efficiency and release of clindamycin in microsponge based gel |
publisher |
Nature Portfolio |
publishDate |
2021 |
url |
https://doaj.org/article/75666214f3064538b3f954124ee4207e |
work_keys_str_mv |
AT alaakhattab optimizationofentrapmentefficiencyandreleaseofclindamycininmicrospongebasedgel AT abdulhakimnattouf optimizationofentrapmentefficiencyandreleaseofclindamycininmicrospongebasedgel |
_version_ |
1718372080605462528 |