{"title":"Choc-Tadalafil Fusion: Unlocking Solubility and Taste Harmony with β-CD-Infused Medicated Chocolate.","authors":"Chetna Modi, Manobika Sinha, Vaishali Thakkar, Hardik Rana, Dipika Chavda","doi":"10.2174/0126673878280254240312053406","DOIUrl":null,"url":null,"abstract":"<p><strong>Objective: </strong>The primary limitations of tadalafil in treating erectile dysfunction are its low solubility and unpleasant bitter taste, which ultimately result in inadequate patient adherence. The present study aimed to develop and characterize a medicated chocolate formulation containing Tadalafil and β-CD (solubility enhancer) employing the concept of Design of Experiment (DoE) using chocolate as a user-friendly excipient.</p><p><strong>Methods: </strong>An inclusion complex was formulated by incorporating the drug into β-CD using the kneading method for solubility improvement and also as a taste masker for Tadalafil. The ratio of drug: β-CD inclusion complex was selected based on a phase solubility study. The inclusion complex was molded into a chocolate base and optimized using the DoE approach. Further, drug excipient interaction was evaluated by DSC and FTIR study.</p><p><strong>Results: </strong>Phase solubility study suggested a 1:1 ratio of Tadalafil: β-CD for better solubility. DSC spectra suggested the conversion of crystalline structure into an amorphous state which indicates improvement of the drug solubility. DSC and FTIR studies revealed that there was no significant interaction between drug and excipients. Next, %CDR (cumulative drug release) at 30 min revealed the immediate effect of Tadalafil from chocolate formulation and free drug analysis (an unbound drug with β-CD) proved reduced bitterness of the drug in the complex. Additionally, the medicated chocolate was found to be stable at room temperature as per stability study.</p><p><strong>Conclusion: </strong>β-CD was found to be a promising multifunctional excipient as a solubility enhancement carrier and taste masker for bitter-tasting drugs.</p>","PeriodicalId":94352,"journal":{"name":"Recent advances in drug delivery and formulation","volume":" ","pages":"110-119"},"PeriodicalIF":0.0000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Recent advances in drug delivery and formulation","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/0126673878280254240312053406","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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Abstract
Objective: The primary limitations of tadalafil in treating erectile dysfunction are its low solubility and unpleasant bitter taste, which ultimately result in inadequate patient adherence. The present study aimed to develop and characterize a medicated chocolate formulation containing Tadalafil and β-CD (solubility enhancer) employing the concept of Design of Experiment (DoE) using chocolate as a user-friendly excipient.
Methods: An inclusion complex was formulated by incorporating the drug into β-CD using the kneading method for solubility improvement and also as a taste masker for Tadalafil. The ratio of drug: β-CD inclusion complex was selected based on a phase solubility study. The inclusion complex was molded into a chocolate base and optimized using the DoE approach. Further, drug excipient interaction was evaluated by DSC and FTIR study.
Results: Phase solubility study suggested a 1:1 ratio of Tadalafil: β-CD for better solubility. DSC spectra suggested the conversion of crystalline structure into an amorphous state which indicates improvement of the drug solubility. DSC and FTIR studies revealed that there was no significant interaction between drug and excipients. Next, %CDR (cumulative drug release) at 30 min revealed the immediate effect of Tadalafil from chocolate formulation and free drug analysis (an unbound drug with β-CD) proved reduced bitterness of the drug in the complex. Additionally, the medicated chocolate was found to be stable at room temperature as per stability study.
Conclusion: β-CD was found to be a promising multifunctional excipient as a solubility enhancement carrier and taste masker for bitter-tasting drugs.
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