Development and Evaluation of Floating Microspheres of Anticonvulsant Drug by 3&lt;sup&gt;2&lt;/sup&gt; Full Factorial Design

bhise, ManishBHISE Ramesh; Sudke, Suresh G.; Burakle, Pramod V.

doi:10.4274/tjps.galenos.2021.53050

Cited by 3 publications

(1 citation statement)

References 13 publications

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“…The floating time of the microspheres was evaluated along with the drug release studies in the dissolution media to know the behaviour of the formulation [19].…”

Section: Floating Timementioning

confidence: 99%

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

PRAGALLAPATI,

LAKSHMI PONNURI,

MURTHY KOLLAPALLI

2023

Int J App Pharm

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Objective: To develop floating microspheres for the topotecan in order to prevent its onversion into inactive carboxylate form in intestinal pH conditions so as to improve its bioavailability. Methods: Chitosan-based porous floating microspheres containing sodium bicarbonate by coacervation technique were developed. Quality by design approach using Box-Behnken Design was adopted to assess the influences of selected formulation variables and their importance on the quality of the finished product. Results: The selected model was analyzed and optimized. The microspheres floated immediately without any lag time upon addition into water and remained floatable for more than 24 h-1. The optimized formulation was found to have the particle size of 379.2 µm, entrapment efficiency of 76.3% and the drug release rate constant of 0.29 h i.e., the release was extended up to 16 h-1. Conclusion: The results affirmed that controlled-release porous microspheres of Topotecan with inherent floating without lag were successfully developed.

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“…The floating time of the microspheres was evaluated along with the drug release studies in the dissolution media to know the behaviour of the formulation [19].…”

Section: Floating Timementioning

confidence: 99%

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

PRAGALLAPATI,

LAKSHMI PONNURI,

MURTHY KOLLAPALLI

2023

Int J App Pharm

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Experimental Investigation on Efficacy of Eudragit RS 100 Polymer in Prolonging Glibenclamide Release by Intragastric Floating Microsphere Formulation and Physicochemical Evaluation

Tripathi,

Yadav,

Mishra

et al. 2024

MNS

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Background:: The amalgamation of targeted transportation and enhancement of the release profile of the active pharmaceutical ingredient is a contemporary trend in the evolution of oral medicinal products. A renowned method to actualize this concept is to develop floating gastroretentive delivery systems that ensure an extended stay of the dosage form on the gastric surface. The success of drug delivery is largely dependent on the type of polymer used that sustains the release and avoids any toxic effects. Intragastric floating drug delivery systems are designed to remain buoyant in the stomach without affecting the gastric emptying rate for a prolonged period. This allows for a slow release of the drug in the stomach, which can be particularly beneficial for drugs with a narrow absorption window, like Glibenclamide, an anti-diabetic medication. Objective:: The current research focused on the sustained drug delivery of Glibenclamide as intragastric floating microspheres. The goal was to adjust the floatation and drug release pattern using Eudragit RS 100 and magnesium stearate as a droplet stabilizer. Different batches of floating microspheres were optimized based on the polymer, drug-polymer concentration, and the amount of magnesium stearate. The strategy aimed to enhance the effectiveness of Glibenclamide, particularly for individuals with diabetes, by facilitating a controlled and consistent release of the drug in the gastric environment. Material and Method:: The solvent evaporation method was used to create four batches of intragastric microspheres. The maximum absorbance of the drug, also known as lambda max, was observed at 212 nm. The prepared batches were evaluated for various in-vitro physicochemical parameters. The average particle size was found to be 619 nm. Rheological studies indicated excellent flow properties. The microspheres exhibited in-vitro buoyancy for up to 7 hours Result:: The entrapment efficiency was as high as 93.19%. Scanning Electron Microscopy (SEM) analysis revealed that the microspheres have a porous structure, which allows for the easy movement of solvents and solutes into and out of the microspheres. Differential Scanning Calorimetry (DSC) and Thermogravimetric Analysis (TGA) indicated the physical and chemical properties of the microspheres. All in-vitro drug release and kinetic studies for the optimized batch (F-M4) revealed that Eudragit RS 100 effectively sustained the intragastric delivery of Glibenclamide. Conclusion:: Floating drug delivery systems enhance oral dosage forms and the range of APIs by ensuring targeted gastric delivery and modified release. This improves bioavailability, reduces drug losses, and partially mitigates side effects.

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An Up-to-Date Review: Microspheres as a New Drug Delivery System

DESNITA,

NOVIANA,

ZAI

et al. 2023

Int J App Pharm

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The application of microsphere systems in drug preparations has seen a significant increase in recent years for various purposes. Microsphere systems can be utilized in a range of drug preparations, utilizing polymer types that are appropriate for the intended release target. Microspheres offer numerous benefits and can be used in various applications, including spacer applications, medication administration, and medical diagnostics. Microspheres have minimal negative effects, a more extended therapeutic effect, require fewer doses, and provide more consistent medication absorption. Additionally, they are adaptable, offer effective encapsulation, and are cost-effective. This overview was compiled to provide an up-to-date summary of the latest developments in new drug delivery systems utilizing microsphere dosage forms. Literature from Scopus, ScienceDirect, and PubMed from 2019 to 2022 was searched to provide the latest information. The use of microsphere systems is categorized into various new drug delivery routes, including gastroretentive, colon, nasal and pulmonary, parenteral, ocular, and topical applications.

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Development and Evaluation of Floating Microspheres of Anticonvulsant Drug by 3<sup>2</sup> Full Factorial Design

Cited by 3 publications

References 13 publications

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

Experimental Investigation on Efficacy of Eudragit RS 100 Polymer in Prolonging Glibenclamide Release by Intragastric Floating Microsphere Formulation and Physicochemical Evaluation

An Up-to-Date Review: Microspheres as a New Drug Delivery System

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