Design and in vitro characterization of buccoadhesive tablets of timolol maleate

Abstract

Objective: The purpose of this work was to develop and evaluate buccoadhesive tablets of timolol maleate (TM) due to its potential to circumvent the first-pass metabolism and to improve its bioavailability.

Methods: The tablets were prepared by direct compression using two release modifying polymers, Carbopol 974P (Cp-974p) and sodium alginate (SA). A 3² full factorial design was employed to study the effect of independent variables, Cp-974p and SA, in various proportions in percent w/w, which influences the in vitro drug release and bioadhesive strengths. Physicochemical properties of the drug were evaluated by ultraviolet, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffraction (P-XRD). Tablets were evaluated for hardness, thickness, weight variation, drug content, surface pH, swelling index, bioadhesive force and in vitro drug release.

Results: The FTIR and DSC studies showed no evidence of interactions between drug, polymers and excipients. The P-XRD study revealed that crystallinity of TM remain unchanged in optimized formulation tablet. Formulation F9 achieves an in vitro drug release of 98.967% ± 0.28 at 8 h and a bioadhesive force of 0.088 N ± 0.01211.

Conclusion: We successfully developed buccal tablet formulations of TM and describe a non-Fickian-type anomalous transport as the release mechanism.

• Buccal
• compatibility
• drug release
• DSC
• entrapments
• FTIR
• P-XRD
• swelling index

Acknowledgements

The authors are thankful to FDC Ltd, Mumbai, India, for providing TM as gift sample. The authors are grateful to MGV’s College of Pharmacy, Nashik, India, for providing necessary facilities to carry out this work. The authors like to thank to Mr. Mahendra Gaikwad and Dr. Prakash Kshirsagar for their help in improving the quality of this article.

Declarations of interest

The authors report no conflicts of interest.