Electrospinning Fibres Mucoadhesive Buccal Tablet using Atorvastatin Calcium Trihydrate as modeling drug: Preparation and Characterization
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Abstract
Atorvastatin (ATV) is a synthetic lipid-lowering agent. According to the Biopharmaceutical Classification System (BCS), ATV is classified as a Class II compound characterized by low solubility and high permeability. Its oral bioavailability is relatively low, at 14%, due primarily to pre-systemic clearance within the gastrointestinal mucosa as well as extensive first-pass metabolism in the liver.
So, this research aimed to develop mucoadhesive tablets containing atorvastatin as fibres via the electrospinning technique for buccal application, aiming to reduce gastric irritation, first-pass metabolism, and enhance bioavailability. Then, three fiber formulations with constant amounts of atorvastatin (ATV) and polyvinyl pyrrolidine, which represent one part and four parts, respectively, and different ratios of soluplus (1:4:1, 1:4:2, 1:4:3) were prepared. They underwent different characterization tests such as Fourier transform infrared spectroscopy, differential scanning calorimetry, optical microscopic imaging, and scanning electron microscopy. The F1 fiber with a ratio of 1:4:1 formulation was further investigated and formulated into mucoadhesive buccal tablets. These tablets underwent various tests, showing satisfactory results. Fourier transform infrared spectroscopy and differential scanning calorimetry studies were harmonized by revealing the change that affirmed the hydrogen bonds more likely to be between ATV and polymers, which assured the amorphous form of fibers by differential scanning calorimetry. F1 fibers achieved 99.6% release of ATV, while F2 and F3 reached 49% and 38.97%, respectively. Also, fibers were examined under an optical microscope, and a scanning electron microscope showed successful fiber formulation and smooth surfaced fibers without any beads or drug crystals on the surface, respectively. Using a controlled flow pump, the buccal tablets (B1 and B2) containing fibers equivalent to 20 mg of ATV showed a slow release of 2.78 mg and 4.39 mg, respectively. In contrast, dissolution by a conventional method, B2 tablet, reached 11.28 mg within 4 hours. In conclusion, drug-loaded ATV fibers with the more stable amorphous form were successfully formulated and characterized, as demonstrated by FTIR and DSC. SEM images exposed fibers with a smooth surface without solid particles, and the successful formation of unidirectional buccal tablets.
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