Development of novel pH–responsive dual crosslinked hydrogel beads based on Portulaca oleracea polysaccharide-alginate-borax for colon specific delivery of 5-fluorouracil

Asnani, Geet P.; Bahekar, Jagan; Kokare, Chandrakant

doi:10.1016/j.jddst.2018.09.023

Cited by 47 publications

(15 citation statements)

References 33 publications

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“…Results showed that Portulaca mucilage and microbead-encapsulated 5-FU formulations were less cytotoxic towards the cell line tested compared to the un-encapsulated drug. It is known that Portulaca is a plant with unique anticancer properties [34]. Therefore, combination of the extract of this plant with 5-FU provides a synergistic mechanism of action, as attested by the data obtained in this study (Figure 2).…”

Section: Cytotoxicity Studiessupporting

confidence: 78%

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In vitro and in vivo evaluation of colon cancer targeted epichlorohydrin crosslinked Portulaca-alginate beads

Asnani

Kokare

2018

Biomolecular Concepts

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The aim of this study was to formulate a novel dual crosslinked hydrogel bead using Portulaca mucilage for colon-targeted delivery of 5-fluorouracil (5-FU) and evaluate its safety, specificity and efficacy. The ionotropic gelation technique was employed to prepare the hydrogel beads of Portulaca mucilage. For this, the mucilage was initially crosslinked with alginate and calcium ions. Epichlorohydrin was employed as a crosslinker in the second crosslinking step. The formulation was subjected to in vitro and in vivo studies to evaluate morphology, size, cytotoxicity, and organ distribution. Human HT-29 colon cancer cell-line was used for in vitro assays and in vivo studies were performed in Wistar rats to assess the usefulness and effectiveness of the formulation for colon cancer therapy. Microsphere sizes ranged from 930 to 977μm and possessed a high level of drug encapsulation efficiency (ca. 78% w/w). Compared with 5-FU solution (Tmax = 1.2 h, mean resident time: MRT = 3.3h) the dual crosslinked Portulaca microspheres exhibited sustained drug release after oral administration to rats (Tmax = 16h, MRT = 14h). The relative bioavailability of 5-FU solution and the microspheres were 100 and 93.6% respectively. Tissue distribution studies indicated high concentration of 5-FU in colon. In-vitro anticancer assay demonstrated IC50 value of 11.50 μg/ml against HT-29 colon cancer cell line. The epichlorohydrin cross-linked Portulaca microspheres prepared in this study provided sustained release of 5-FU up to 16h in the colonic region and enhanced the antitumor activity of the neoplastic drug. The formulation is hence an ideal carrier system for colon-targeted drug delivery.

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Section: Cytotoxicity Studiessupporting

confidence: 78%

“…calcium alginate [33]. Recently, it has been reported that single crosslinked formulations show premature drug release [34]. Consequently, in order to extend the release of drug in the colon the single crosslinked beads were crosslinked again using epichlorohydrin (a bifunctional alkylating agent).…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo evaluation of colon cancer targeted epichlorohydrin crosslinked Portulaca-alginate beads

Asnani

Kokare

2018

Biomolecular Concepts

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“…The controlled caffeine release from the prepared samples was carried out at 37°C in two media during a 24 hours period: 0.2 M phosphate buffer (pH = 6.8) (PB) (as a simulation of duodenum pH environment) and 0.1 M solution of HCl (as a simulation of stomach pH environment). [ 31 ] The absorbances of the solutions were measured at predefined time intervals at 273 nm using the UV‐Vis Shimadzu UV‐1800 spectrophotometer. To provide perfect sink conditions during the caffeine release, each synthesized controlled release system was put into 100 mL of a prepared media.…”

Section: Methodsmentioning

confidence: 99%

Modification of hydrophilic polymer network to design a carrier for a poorly water‐soluble substance

Markovič

Panic

Šešlija

et al. 2020

Polymer Engineering & Sci

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pH sensitive, nontoxic, and biocompatible poly(methacrylic) acid (PMAA) based soft networks have been extensively used in the design of systems for targeted drug delivery. Still, their highly hydrophilic nature limits their potential to be used as a carrier of poorly water-soluble substances. With the aim to overcome this limitation, the present study details a new approach for modification of PMAA based carriers using two amphiphilic components: casein and liposomes. The FTIR analysis revealed structural features of each component as well as the synergetic effect that originated from the formation of specific interactions. Namely, hydrophobic interactions between the poorly watersoluble model drug (caffeine) and casein enabled caffeine encapsulation and controlled release, while addition of liposomes ensured better control of the release rate. The morphological properties of the carriers, swelling behavior, and release kinetics of caffeine were investigated depending on the variable synthesis parameters (neutralization degree of methacrylic acid, concentration of caffeine, presence/absence of liposomes) in two different media simulating the pH environment of human intestines and stomach. The data obtained from in vitro caffeine release were correlated and analyzed in detail using several mathematical models, indicating significant potential of investigated carriers for targeted delivery and controlled release of poorly water-soluble substances.

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“…Sodium alginates are known to be biocompatible, biodegradable, and ‘Generally Recognized as Safe (GRAS)’ with no reports about serious adverse effects of alginates as food additives [ 90 ]. Toxicology studies on sodium alginate were carried out very early in the 1940s using lab animals such as mice, rabbits, and even cats [ 91 , 92 ].…”

Section: Algal Hydrocolloidsmentioning

confidence: 99%

Algae-derived hydrocolloids in foods: applications and health-related issues

et al. 2021

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Hydrocolloids are a class of food additives with broad applications in the food industry to develop structure in food ingredients. Hydrocolloids can be synthetic, plant-based, or animal-based. Increasing consumer awareness has led to the use of natural food ingredients derived from natural sources, making algae-derived hydrocolloids more appealing nowadays. Algae-derived hydrocolloids such as carrageenan, agar, and alginate are widely used in the food industry as thickening, gelling, and emulsifying agents. Carrageenans are sulfated polysaccharides with diverse structural specificities. The safety of carrageenan use in the food industry has been widely debated recently due to the reported pro-inflammatory activities of carrageenan and the probable digestion of carrageenan by the gut microbiota to generate pro-inflammatory oligosaccharides. In contrast, both agar and alginate are primarily nontoxic, and generally no dispute regarding the use of the same in food ingredients. This review provides an overview of the algae industry, the food additives, the algae-derived hydrocolloids, the applications of algae-derived hydrocolloids in food industries, health-related studies, and other sectors, along with future perspectives. Even though differences of opinion exist in the use of carrageenan, it is continued to be used by the food industry and will be used until suitable alternatives are available. In summary, algal hydrocolloids are 'label-friendly' and considered a safe option against synthetic additives.

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Development of novel pH–responsive dual crosslinked hydrogel beads based on Portulaca oleracea polysaccharide-alginate-borax for colon specific delivery of 5-fluorouracil

Cited by 47 publications

References 33 publications

In vitro and in vivo evaluation of colon cancer targeted epichlorohydrin crosslinked Portulaca-alginate beads

In vitro and in vivo evaluation of colon cancer targeted epichlorohydrin crosslinked Portulaca-alginate beads

Modification of hydrophilic polymer network to design a carrier for a poorly water‐soluble substance

Algae-derived hydrocolloids in foods: applications and health-related issues

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