Clotrimazole nanoemulsion for malaria chemotherapy. Part I: Preformulation studies, formulation design and physicochemical evaluation

Clotrimazole was formulated in nanoemulsion based system with the aim of improving its solubility and dissolution, which can further used for its preclinical evaluation. Clotrimazole nanoemulsion was prepared using spontaneous nanoemulsification method. Preformulation studies were preformed to evalu...

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Bibliographic Details
Published in:International journal of pharmaceutics 2012-07, Vol.431 (1-2), p.138-148
Main Authors: Borhade, Vivek, Pathak, Sulabha, Sharma, Shobhona, Patravale, Vandana
Format: Article
Language:English
Subjects:
Antimalarials - chemistry
Chemistry, Pharmaceutical
chemotherapy
Chromatography, High Pressure Liquid
Clotrimazole
Clotrimazole - chemistry
drugs
emulsifying
Emulsions
Excipients - chemistry
Hydrogen-Ion Concentration
malaria
Nanoemulsion
nanoemulsions
Nanostructures - chemistry
oils
Phase behaviors
Preformulation
Solubility
Stability
Surface-Active Agents - chemistry
surfactants
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Summary:Clotrimazole was formulated in nanoemulsion based system with the aim of improving its solubility and dissolution, which can further used for its preclinical evaluation. Clotrimazole nanoemulsion was prepared using spontaneous nanoemulsification method. Preformulation studies were preformed to evaluate drug-excipient compatibility, solution state pH stability and pH solubility profile. Solubility of clotrimazole in oils, surfactants and cosurfactants was determined to identify nanoemulsion components. Surfactants and cosurfactants were screened for their ability to emulsify selected oily phases. Phase diagrams were constructed to identify area of nanoemulsification. Influence of clotrimazole and pH of dilution medium on phase behavior were assessed. Drug-excipient chemical compatibility study facilitated to anticipate acid catalyzed degradation of clotrimazole. The pH of nanoemulsion was adjusted to 7.5, which could stabilize clotrimazole. Nanoemulsion composed of Capryol 90, Solutol HS 15 and Gelucire 44/14 enhanced solubility of clotrimazole up to 25mg/ml. The optimized clotrimazole nanoemulsion could withstand the extensive dilution and did not show any phase separation or drug precipitation. The nanoemulsion exhibited mean globule size
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2011.12.040