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.
Highlights
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
CLN is commercially available as CLN-HCl and CLN-PO4, Both of which are freely soluble in water, and it is a challenging task to incorporate them into microsponges via quasi emulsion solvent diffusion method, as high amounts of the freely soluble drug would leach into the external aqueous phase during formulation and lead to low drug e ntrapment[9]
All formulations revealed high EE% and PY%, which could be attributed to the porous structure of the microsponge formulations
Summary
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, conversion of the hydrochloride salt to free base was done. Microsponges would control the drug delivery, enhance the drug tolerability, and reduce the frequency of application while still sustaining the efficacy of the drug They could absorb sebaceous secretions which are highly found on the skin of most acne patients without cause drying. CLN is commercially available as CLN-HCl and CLN-PO4, Both of which are freely soluble in water, and it is a challenging task to incorporate them into microsponges via quasi emulsion solvent diffusion method, as high amounts of the freely soluble drug would leach into the external aqueous phase during formulation and lead to low drug e ntrapment[9]
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