Abstract
Objective: The present research work aims at describing the formulation and evaluation of the ocular delivery system of moxifloxacin hydrochloride (MH) based on the concept of ion sensitive in situ gelations.Methods: In situ gel was prepared by a hot method using 0.6% of gelrite, 0.25% hydroxypropylmethylcellulose (HPMC K4M) and 0.023% tamarind gum as bioadhesive polymers for sustained drug release. Optimization was done by Box Behnken Design with different concentration of gelrite (X1), HPMC K4M (X2) and tamarind gum (X3) as independent variables. In situ gel was optimized based on mucoadhesion index (Y1), Gel strength (Y2) and in vitro drug release (Y3). Influence of the quantitative variable on the dependent variable was predicted by a polynomial equation.Results: Infrared spectroscopy excluded any interaction between drug and excipients. The selected independent variables significantly influenced the responses and were able to sustain the drug release. The prepared gel with a pH of 6.8 to 7.4 exhibited non-newtonian flow with no ocular irritation. The formulation remained stable with no change in pH and viscosity after 30 d of stability study.Conclusion: Thus, moxifloxacin hydrochloride (MH) in situ gel is a viable alternative to a conventional delivery system with the properties of sustained drug release, prolonged ocular retention, and improved corneal penetration.
Highlights
Development of suitable drug delivery systems for ocular therapy is one of the major problems being faced by pharmaceutical scientists
Pure moxifloxacin hydrochloride (MH) spectra showed characteristic peaks represented as C =O stretching vibrations shown at 1709 cm-1, N-H stretching vibrations at 2949 cm-1, O-H stretching vibration at 3530 cm-1
The Fourier transforms infrared spectroscopy (FTIR) spectrums of physical mixture revealed the main absorption bands of moxifloxacin hydrochloride with no significant changes compared with the spectrum of pure drug
Summary
Development of suitable drug delivery systems for ocular therapy is one of the major problems being faced by pharmaceutical scientists. Conventional ocular dosage forms result in poor bioavailability due to tear production, nonproductive absorption, transient residence time, and impermeability of corneal epithelium. These physiological and anatomical constraints deliver only a small fraction of the instilled dose of ocular therapeutics and less than 1% is effectively absorbed and reaches the internal anterior tissue of the eyes [2]. Several methods for prolonging the contact time between drug and corneal–conjunctival epithelium are investigated to increase the drug bioavailability Various ophthalmic products, such as inserts, ointments, suspensions, and aqueous gels, have been developed to enhance ophthalmic bioavailability. These ocular drug delivery systems, have not been used extensively because of some drawbacks, such as blurred vision and poor patient compliance
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