Abstract

Objective: In the current research work, dipyridamole, a BCS class–II drug, was aimed to be formulated as floating controlled release microballoons using ethyl cellulose as polymer and span 80 as surfactant to improve the gastric retention of drug as the multi-particulate dosage forms have tremendous advantages over single unit dosage forms.
 Methods: Microballoons were prepared by the emulsion solvent evaporation method. Prepared microballoons were characterized for entrapment efficiency, particle size, floating behavior and drug release studies. The study of effect of various formulation and process parameters like surfactant concentration, solvent volume, the volume of internal phase, polymer concentration, rotation speed on the drug entrapment efficiency and particle size of the microballoons were carried by using Box–Benhken to optimize the formulated microballoons.
 Results: The smallest particle size of the microballoons was found to be 205.9 µm in the F32 formulation. The highest drug entrapment efficiency was found to be 93.4% in the F34 formulation. Buoyancy studies showed all the formulations have good floating characteristics that lasted for a minimum of 24 h. The maximum yield of microballoons was found in the F7 formulation with 91.8% yield. The final results were statistically treated using ANOVA and were found to be significant (p value<0.05).
 Conclusion: Thus, the obtained results and their statistical interpretations indicated floating microballoons of dipyridamole were formulated effectively.

Highlights

  • Oral controlled release dosage forms have the potential to upkeep an effective concentration in the system for a longer duration

  • The results of the percentage yield of dipyridamole microballoons were showed in table 2

  • All the formulations of microballoons were prepared by the solvent evaporation technique and from the results, more than 76.4% yield was observed in any case, which indicated that the solvent evaporation technique, along with the selected experimental conditions was highly effective for the preparation of floating microspheres

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Summary

Introduction

Oral controlled release dosage forms have the potential to upkeep an effective concentration in the system for a longer duration. It provides ease in dosage administration to the patient but the benefits are yet obstructed due to the short gastric retention time (GRT) and the unpredictable rapid gastric rate may cause partial drug release in the absorption zone of the patient’s body hampering the efficiency of the dosage It has caused awaited development in oral gastroretentive drug delivery systems (GRDDS) [1]. Uniform distribution of the multi particulate dosage in the gastric content could result in more reproducible absorption and a reduced risk of local irritation than single-unit dosage forms Such prolonged gastric retention controls the time and the space in the stomach by maintaining the delivery system positioned at a steady site and thereby properly delivering the drug

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