Assessing the bioadhesivity of Acconon MC 8-2 EP/NF for gastroretention of floating microsponges of loratadine and achieving controlled drug delivery

Singh, Sumita; Pathak, Kamla

doi:10.18869/acadpub.pbr.2.2.58

Cited by 11 publications

(7 citation statements)

References 10 publications

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“…Optimisation by QBD for preparing microparticulate systems is nowadays practised by formulation scientists, and optimised operating variables aid in scale-up design. To enhance reliability and reproducibility of the method, several investigators started attempting simple factorial design [29], Central Composite Design -RSM method by design expert software [1,11,13,16,[28][29][30][31]. They presented linear as well as quadratic models.…”

Section: Introductionmentioning

confidence: 99%

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Halder

Poddar²,

Khanam

2021

Preprint

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The present investigation aims at developing models by response surface methodology (FCCCD) followed by the scale-up method in preparing control release microsponge particles loaded with 5- fluorouracil, a drug used to treat actinic keratosis and colon cancer, and producing a new Dermal Delivery System. The polymer-based (ethyl cellulose and eudragit RS 100) microsponge particles were prepared by the w/o/w double emulsification method. The optimized product was formed with the combination of independent variables levels: polymer (600 mg), stirring speed (1198 rpm) and surfactant (2% w/v), yielding responses as yield (~63.6257%), the average size of particles (~151.563 µm), entrapment efficiency (~75.319 %) and drug release in 8hr (~75.75%), with desirability value of 0.737. The products showed similar responses as obtained in scale-up work. FT-IR, DSC and SEM studies confirmed the drug's compatibility with polymers and porous morphology. Finally, gel embedded optimised product showed shear-thinning rheological property, ideal for drug release from the thixotropic gel.

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Section: Introductionmentioning

confidence: 99%

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Halder

Poddar²,

Khanam

2021

Preprint

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“…The gastric floating microsponge of curcumin developed using the two polymers eudragit and ethylcellulose together by Arya et al demonstrated a drug release of 88.4 to 90.8% of curcumin after 8 hours of the release study [26]. In another study reported by Singh et al, the cumulative drug release values obtained for the loratadine gastric floating microsponge prepared using ethylcellulose alone were comparatively slightly lower numbers 66.75 to 88.15% drug release [27] and in one more study, it is reported that cinnarizine release from the gastric floating microsponge was far less and it was between 57.9 and 88.7% at the end of same 8 hours [28]. However, on increasing the duration of the in vitro drug release study from 8 to 12 hours and with the use of both the polymers eudragit and ethylcellulose together in the microsponge preparation it was noticed that the drug release was almost complete as reported by Chargonda et al [29].…”

Section: Critical Factors Affecting Microsponge and Microsphere Efficacymentioning

confidence: 99%

“…Zero-order release was the best fit kinetic model for the microsponges developed with anyone polymer ethylcellulose or eudragit and dichloromethane alone as a solvent [29]. It is thus clear that the variation in the drugs release from the floating microsponges of curcumin [26], cinnarizine [28], famotidine [29], and loratadine [27] are related to the polymeric and solvent composition of each type of gastric floating microsponges. As far as the release mechanisms are concerned, all floating microsponges exhibited drug release governed by Fickian diffusion mechanisms [26,27], except to lower concentration of eudragit and it was governed by diffusion and swelling mechanisms [27].…”

Section: Critical Factors Affecting Microsponge and Microsphere Efficacymentioning

confidence: 99%

The Impact of Microsponge and Microsphere on Improving Oral Bioavailability of Medications: A Short Review

Alshehry¹

2022

J Pharm Res Sci Technol

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While many diseases require an efficient drug delivery technology that has the ability to improve bioavailability and alleviate side effects, various types of gastroretentive drug delivery systems (GRDDS) have been developed in order to overcome the obstacles, which are related to a narrow absorption window, instability, site of action, side effects, and dosing frequency. In this context, microsponge and microsphere systems depict two different types of GRDDS, aiming to provide adequate time for active ingredients to be absorbed in the stomach despite the variation in releasing mechanisms of the entrapped ingredients. For the successful designing of these systems, it is essential to optimize the characterizations of the formulated microparticles by considering physiological, pharmaceutical, and patient-related factors, which have a dramatic impact on the efficacy. Consequently, they will demonstrate different behaviors at the desired site of action, determining which systems are showing superiority compared to others. However, each microparticle system has some advantages over the others, providing more options for researchers to ease the difficulties that exist with conventional oral dosage forms. Therefore, this review aims to shed the light on critical factors that have significant impacts on microsponge and microsphere systems and addresses their advantages and disadvantages, providing an understanding of these criteria in order to optimize the drug systems.

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“…When compared to the aqueous medium the system offers lower bulk density that helps the drug de-livery system to float in the gastric fluid. Several approaches like mucoadhesive system, swelling system, high density system, magnetic system and floating system have been developed to increase the residence time of drug in stomach [7][8][9].…”

Section: Introductionmentioning

confidence: 99%

Development and Optimization of Methscopolamine Bromide Gastroretentive Floating Tablets Using 32 Factorial Design

Singh

Kumar

Shankar³

2020

Drug Res (Stuttg)

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Purpose The aim of this study was to formulate methscopolamine floating drug delivery system to increase its gastro retention for further enhancement of absorption and overall bioavailability. Method Direct compression method was used to formulate floating drug delivery system of methscopolamine bromide. Different amount of HPMC, PVP K25, and MCC were used for preparation of tablets. Result The prepared tablets were evaluated for thickness, hardness, weight variation, floating lag time, swelling index and in-vitro drug release. All the formulations showed less than 10% of weight variation. The hardness and thickness of all the formulations were within the range of 3.7−4.2 kg/cm2 and 3.63−3.83 mm respectively. Floating lag time for all the formulations was reported in seconds. The degree of swelling was reported in range of 82.10−85.83%. In vitro release was carried out for 24 h. The maximum release was shown by F1 (93.947%) while the minimum release was observed for F4 (90.420%). The best formulation was optimized on the basis of percentage cumulative drug release, floating lag time and swelling index. F1 found to be the best formulation. Further on analyzing the drug release mechanism, F1 found to exhibit korsmeyer peppas model of drug release. Conclusion Floating gastroretentive tablet of methscopolamine bromide was successfully developed using direct compression method with potential to enhance the drug absorption and effective treatment of peptic ulcer.

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Assessing the bioadhesivity of Acconon MC 8-2 EP/NF for gastroretention of floating microsponges of loratadine and achieving controlled drug delivery

Cited by 11 publications

References 10 publications

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

The Impact of Microsponge and Microsphere on Improving Oral Bioavailability of Medications: A Short Review

Development and Optimization of Methscopolamine Bromide Gastroretentive Floating Tablets Using 32 Factorial Design

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