Abstract

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time.
 Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies).
 Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h.
 Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

Highlights

  • Oral route of administration is one of the most suitable and generally used method of drug administration and the development of stomach specified oral controlled release drug delivery system is difficult due to the difference in pH in different sections of the gastrointestinal tract, the alteration in gastric emptying time and the problem of localizing an oral delivery system in a selected location of the gastrointestinal tract

  • Drug and polymer (HPMC K4M, carbopol 940, and Ethylcellulose) in various proportions were dissolved in a 20 ml acetone which was placed in a small beaker with a magnetic bead on the magnetic stirrer at room temperature

  • In this research, floating microspheres of ciprofloxacin were prepared by carbopol 940, ethylcellulose, and hydroxypropylmethyl cellulose (HPMC K4M) by the solvent evaporation method

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Summary

Introduction

Oral route of administration is one of the most suitable and generally used method of drug administration and the development of stomach specified oral controlled release drug delivery system is difficult due to the difference in pH in different sections of the gastrointestinal tract, the alteration in gastric emptying time and the problem of localizing an oral delivery system in a selected location of the gastrointestinal tract. Gastroretentive delivery systems are mainly designed for drugs that have a narrow absorption window. Such systems get retain at the site of absorption and release the drug in a controlled manner for a longer time. Drugs that have a short half-life require frequent dosing as they get eliminated quickly from blood circulation to increase the bioavailability of such drugs controlled-release formulations are prepared [2]

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