Abstract
Purpose: To formulate bioadhesive clotrimazole vaginal tablets using natural polymers in order to provide long-term therapeutic action at the site of infection. Methods: The tablets were prepared by direct compression using bioadhesive polymer mixtures: hydroxypropyl methylcellulose/sodium carboxymethylcellulose (HPMC/NaCMC) and HPMC/Guar gum (GG) in different ratios. Differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopic evaluations were carried out to assess compatibility between the drug and the excipients. The tablets were subjected to various pre- and post-compression evaluations, including in vitro drug release, in vitro bioadhesive strength, swelling and stability studies. Results: The results show that all the formulations satisfied Indian Pharmacopoeial specifications for tablet parameters. DSC and FT-IR data indicate there was no interaction between the drug and the excipients. Drug dissolution rate at pH 6.0 followed the rank order: HPMC)/NaCMC > HPMC/GG. There was increase in swelling index with time at 37 0C. The combination of HPMC with NaCMC showed greater mucoadhesive strength and superior controlled drug release to the formulations prepared with GG polymer mixture. Furthermore, the release properties of the former in pH 6.0 buffer, as well as release mechanism (n values), were negligibly affected by ageing. Conclusion: This study indicates the possible use of suitable mixtures of natural and semi-synthetic cellulosic polymers for the preparation of clotrimazole mucoadhesive tablets for application as a vaginal controlled delivery system. Keywords: Clotrimazole, Swelling, Cellulosic polymers, Guar gum, Bioadhesion, Release properties
Highlights
INTRODUCTIONConventional vaginal drug delivery systems (e.g., pessaries, foams, creams, gels and tablets) have some limitations such as leakage, messiness and low residence time, which contribute to poor subject or patient compliance [1]
Conventional vaginal drug delivery systems have some limitations such as leakage, messiness and low residence time, which contribute to poor subject or patient compliance [1]
This study addresses the possible use of a mixture of HPMC in different ratios with NaCMC or Guar Gum (GG) for the preparation of mucoadhesive tablets of clotrimazole, a widely used antifungal agent for vaginal mycotic infections
Summary
Conventional vaginal drug delivery systems (e.g., pessaries, foams, creams, gels and tablets) have some limitations such as leakage, messiness and low residence time, which contribute to poor subject or patient compliance [1]. This study addresses the possible use of a mixture of HPMC in different ratios with NaCMC or GG for the preparation of mucoadhesive tablets of clotrimazole, a widely used antifungal agent for vaginal mycotic infections. Clotrimazole was received free of charge from Zyg Pharma Mumbai, India while sodium caboxymethylcellulose (NaCMC), hydroxypropylmethylcellulose (HPMC) and Guar Gum (GG) (all from Loba Chemie, Mumbai, India) were used as the polymers. Tablets containing 20 % clotrimazole and weighing 500 mg were prepared by direct compression of the formulation in a 10-station tablet machine (minipress-1674, Rimek, India) fitted with round, flat-faced 12 mm punches. A particle size of less than 160 μm for all components was selected to avoid any fractional segregation and the formulation well mixed with a mortar and pestle to obtain a homogenous blend prior to compression
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