Development and in vitro evaluation of coated pellets containing chitosan to potential colonic drug delivery

Ferrari, Priscileila Colerato; Souza, Fagner Magalhães; Giorgetti, Leandro; Oliveira, Giselle F.; Ferraz, Humberto Gomes; Chaud, Marco V.; Evangelista, Raul Cesar

doi:10.1016/j.carbpol.2012.08.044

Cited by 30 publications

(12 citation statements)

References 25 publications

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“…There are defined various shape factors to describe pellets which do separate sperical and nonspherical pellets. One of the most popular shape factor is sphericity (S), which value equal to 1.0 describes a perfect circle (or a perfect sphere) 25,26 . One of the aim of this experiment was to prepare pellets which S close to the ideal value.…”

Section: Resultsmentioning

confidence: 99%

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The development andin vitroevaluation of herbal pellets coated with Eudragit FS 30

Kalėdaitė

Bernatonienė

Dvořáčková

et al. 2014

Pharmaceutical Development and Technology

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The objective of this study was to prepare pellets of thyme (Thymus vulgaris L.), stinging nettle (Urtica dioica L.) and sage (Salvia officinalis L.) dry extracts by extrusion-spheronization technique to improve technological properties and investigate dissolution profiles of pellets covered different levels of pH-sensitive polymer Eudragit® FS. Optimal sample of pellets were prepared using microcrystalline cellulose and lactose as excipients and demonstrated excellent technological quality properties such as Hausner ratio (1.07 ± 0.11) and compressibility index (6.73 ± 0.94%) value, spericity (0.87 ± 0.001) and friability (0.22 ± 0.08 N). Pellets were coated by 10-35% (w/w) of Eudragit® FS. Dissolution studies showed that less than 20% of coating could not prevent dissolution of phenols in pH 1.2, 20% Eudragit® FS coating is enough to prevent herbal extract against dissolution in the stomach. There were observed no statistical significant differences between 20% and 25% or higher amount of coating polymer to a dissolution of phenols in low pH.

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Section: Resultsmentioning

confidence: 99%

“…One of the most important quality parameter of pellets is their circularity or spericity 25,26 . There are defined various shape factors to describe pellets which do separate sperical and nonspherical pellets.…”

Section: Resultsmentioning

confidence: 99%

The development andin vitroevaluation of herbal pellets coated with Eudragit FS 30

Kalėdaitė

Bernatonienė

Dvořáčková

et al. 2014

Pharmaceutical Development and Technology

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“…Chitosan consists of b-(1,4)-linked D-glucosamine units with variable degrees of N-acetylation (Casettari et al, 2012). It has been used for tissue regeneration (Ma et al, 2010;Cooper et al, 2011;Park et al, 2013) and drug delivery applications (Rokhade et al, 2007;Abruzzo et al, 2012;Ferrari et al, 2013) because of its tissue compatibility, biodegradability and low toxicity (Ao et al, 2011;Cooper et al, 2011;Tsai et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo evaluation of thermosensitive chitosan hydrogel for sustained release of insulin

Tahrir¹,

Ganji²,

Mani

et al. 2014

Drug Delivery

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Injectable In situ gel-forming chitosan/b-glycerol phosphate (CS/b-Gp) solution can be introduced into the body in a minimally invasive manner prior to solidifying within the target tissue. This hydrogel is a good candidate for achieving a prolonged drug delivery system for insulin considering its high molecular weight. In addition to the physicochemical characterization of this hydrogel, in vitro and in vivo applications were studied as a sustained insulin delivery system. In the in vitro release studies, 19-63% of total insulin was released from the CS/b-Gp hydrogel within 150 h at different b-Gp and insulin concentrations. The best formulation was selected for in vivo experimentation to control the plasma glucose of diabetic mice models. The hypoglycemic effect of this formulation following subcutaneous injection in diabetic mice lasted 5 d, significantly longer than that of free insulin solution which lasted several hours.

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“…The CINS153, INS205 and CINS205 samples released lower amounts of INS at pH 1.2 (32, 37 and 18%, respectively) and pH 4.5 (14, 22 and 14%, respectively) than in phosphate buffer pH 6.8 (53, 40 and 67% respectively), demonstrating a pH-dependent behavior that can be successfully exploited for the targeted release. Such behavior is related to the influence of pH on the ionization of the anionic polymers, so that in acid media their carboxyl groups are protonated, promoting the electrostatic interaction of the polymer chains, which become tighter and thus hinder the penetration of liquids and the subsequent dissolution/diffusion of drug molecules [49,50].…”

Section: Evaluation Of Protective Effect Of Mp Against Ins Degradationmentioning

confidence: 99%

Retrograded starch/pectin coated gellan gum-microparticles for oral administration of insulin: A technological platform for protection against enzymatic degradation and improvement of intestinal permeability

Meneguin

Beyssac

Garrait

et al. 2018

European Journal of Pharmaceutics and Biopharmaceutics

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Gellan gum microparticles coated with colon-specific films based on retrograded starch and pectin was developed for enhancing the oral release of insulin (INS). The system developed promoted an impressive protection of INS (80%) after 120 min of incubation with trypsin and alpha-chymotrypsin, while only 3% of free INS remained intact after the same time, possibility due to the calcium chelating activity of the polymers in inhibiting the proteolytic activity. In vitro INS release in media simulating the gastrointestinal portions revealed a pH-dependent behavior, as well as the significance of the coating in lowering the release rates in relation to their counterparts. The permeability of INS on Caco-2 cells monolayers and excised rat intestine were significantly improved, mainly due to the influence of the anionic polymers on tight junctions opening, along with the excellent mucoadhesive properties of the gellan gum. All these features together contributed greatly to the hypoglycemic effect observed after the oral administration of the INS-loaded MP in diabetic rats, with reduction of up to 51% of blood glucose levels. The important findings of this work should contribute to the advances about the search of alternatives for oral administration of INS.

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Development and in vitro evaluation of coated pellets containing chitosan to potential colonic drug delivery

Cited by 30 publications

References 25 publications

The development andin vitroevaluation of herbal pellets coated with Eudragit FS 30

The development andin vitroevaluation of herbal pellets coated with Eudragit FS 30

In vitro and in vivo evaluation of thermosensitive chitosan hydrogel for sustained release of insulin

Retrograded starch/pectin coated gellan gum-microparticles for oral administration of insulin: A technological platform for protection against enzymatic degradation and improvement of intestinal permeability

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