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2000
Volume 8, Issue 1
  • ISSN: 2452-2716
  • E-ISSN: 2452-2724

Abstract

Introduction/Background

BCL is a BCS Class III drug. It has a relatively low oral bioavailability of about 40% due to its short half-life (2-4 hours) and rapid clearance from the body. Developing gastroretentive technology can enhance its bioavailability by prolonging its retention in the stomach, ensuring more consistent absorption and therapeutic effects. It is well absorbed in the acidic environment of the stomach (pH 1-4). Due to the highly hydrophilic nature of BCL, the development of hydrocolloid-based floating beads for oral controlled release presents a significant challenge. To overcome this challenge, a blend of Sodium Alginate and Gelucire 43/01 was used which forms an intercalating structure network that helps in controlling drug release in the stomach.

Aim

The aim of this study is to develop and optimize a gastro buoyant drug delivery system of Baclofen (BCL) using a Taguchi 32-factorial design assisted formulation. The formulation encompasses Gelucire 43/01 and sodium alginate to create gastro-buoyant multi-unit systems that provide controlled drug release in the gastric environment.

Objective

To develop and characterize BCL loaded beads matrixed with Gelucire 43/01 and Sodium Alginate to retain in the stomach for achieving site-specific drug delivery. The formulation were investigated to achieve a controlled release of BCL to maintain therapeutic drug level concentration over an extended period, reducing the frequency of dosing. Utilization of 32 factorial designs to investigate the effects of various formulation variables on the buoyancy time (Y) and drug release (Y) profile..

Methodology

09 formulations were prepared as per 32 Taguchi factorial design studies using Minitab software.

Results and Discussion

From conducted optimization studies, it was found that Gelucire 43/01 is responsible for achieving buoyancy and retardation of Baclofen from the intercalating polymeric matrices in 0.1 N HCl. Drug excipient thermal analysis studies confirmed that there is development of polyelectrolyte complex. All the formulations remained buoyant till the time of drug release with 100% buoyancy. Entrapment efficiency ranges from 99.74-90.90 with a low standard deviation. The obtained polynomial quadratic equation indicates the synergistic effect for both the polymers for Y and Y response. % dissolution efficiency ranging from 92.78 to 99.62, which means formulations have potential to produce therapeutic response when given . By using topography studies using SEM, it was found that there is a generation of porous structure which leads to lesser density than the utility (1.04 g/cm3) and is responsible for achieving buoyancy. Formulations F2 and F3 were found to be optimized. Drug release kinetics suggested that all the formulations follow zero-order kinetics with low AIC values. Obtained Durbin-Watson statistics suggested that models are highly validated and the degree of error is less for both responses (Y and Y).

Conclusion

It may be concluded that polymer matrices composed of Gelucire 43/01 and sodium alginate as release retardants may be an excellent carrier for stomach-specific delivery of model drug BCL.

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2025-03-13
2025-09-28

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32 Factorial Designed Baclofen Loaded Gelucire 43/01-Sodium Alginate Gastro-buoyant Multi-unit Systems for Controlled Drug Delivery in Gastric Environment
Curr Appl Polym Sci 8, E24522716362601 (2025); https://doi.org/10.2174/0124522716362601250212100844
/content/journals/caps/10.2174/0124522716362601250212100844
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  • Article Type:     Research Article
Keyword(s): Baclofen; gastro-buoyant; gastroretentive; gelucire 43/01; polyelectrolyte complex; sodium alginate; sustained

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