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Bipolymeric Pectin Millibeads Doped with Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine.
Molecules. 2020 Dec 03; 25(23)M

Abstract

Targeted drug delivery systems are a very convenient method of treating inflammatory bowel disease. The properties of pectin make this biopolymer a suitable drug carrier. These properties allow pectin to overcome the diverse environment of the digestive tract and deliver the drug to the large intestine. This investigation proposed bipolymeric formulations consisting of the natural polymer pectin and a synthetic polymer containing the drug 5-aminosalicylic acid. Pectin beads were prepared via ionotropic gelation involving the interaction between the hydrophilic gel and calcium ions. The obtained formulations consisted of natural polymer, 5-aminosalicylic acid (5-ASA) and one of the synthetic polymers, such as polyacrylic acid, polyvinylpyrrolidone, polyethylene glycol or aristoflex. The release of the drug was carried out employing a basket apparatus (USP 1). The acceptor fluid was pH = 7.4 buffer with added enzyme pectinase to reflect the colon environment. The amount of the released drug was determined using UV-Vis spectrophotometry at a wavelength of λ = 330 nm. The kinetics of the drug dissolution revealed that none of the employed models was appropriate to describe the release process. A kinetic analysis of the release profile during two release stages was carried out. The fastest drug release occurred during the first stage from a formulation containing pectin and polyethylene glycol. However, according to the applied kinetic models, the dissolution of 5-ASA was rather high in the formulation without the synthetic polymer during the second stage. Depending on the formulation, 68-77% of 5-ASA was released in an 8-hour time period. The FTIR and DSC results showed that there was no interaction between the drug and the polymers, but interactions between pectin and synthetic polymers were found.

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Authors+Show Affiliations

Wójcik-Pastuszka D
Department of Physical Chemistry and Biophysics, Faculty of Pharmacy, Wroclaw Medical University, ul. Borowska 211A, 55-556 Wroclaw, Poland.
Potempa A
Department of Physical Chemistry and Biophysics, Faculty of Pharmacy, Wroclaw Medical University, ul. Borowska 211A, 55-556 Wroclaw, Poland.
Musiał W
Department of Physical Chemistry and Biophysics, Faculty of Pharmacy, Wroclaw Medical University, ul. Borowska 211A, 55-556 Wroclaw, Poland.

MeSH

CalciumChemistry, PharmaceuticalDelayed-Action PreparationsDrug CarriersDrug Delivery SystemsGelsHydrogen-Ion ConcentrationHydrophobic and Hydrophilic InteractionsKineticsMesalaminePectinsPolymers

Pub Type(s)

Journal Article

Language

eng

PubMed ID

33287276

Citation

Wójcik-Pastuszka, Dorota, et al. "Bipolymeric Pectin Millibeads Doped With Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine." Molecules (Basel, Switzerland), vol. 25, no. 23, 2020.
Wójcik-Pastuszka D, Potempa A, Musiał W. Bipolymeric Pectin Millibeads Doped with Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine. Molecules. 2020;25(23).
Wójcik-Pastuszka, D., Potempa, A., & Musiał, W. (2020). Bipolymeric Pectin Millibeads Doped with Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine. Molecules (Basel, Switzerland), 25(23). https://doi.org/10.3390/molecules25235711
Wójcik-Pastuszka D, Potempa A, Musiał W. Bipolymeric Pectin Millibeads Doped With Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine. Molecules. 2020 Dec 3;25(23) PubMed PMID: 33287276.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Bipolymeric Pectin Millibeads Doped with Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine. AU - Wójcik-Pastuszka,Dorota, AU - Potempa,Aleksandra, AU - Musiał,Witold, Y1 - 2020/12/03/ PY - 2020/11/05/received PY - 2020/11/24/revised PY - 2020/12/01/accepted PY - 2020/12/8/entrez PY - 2020/12/9/pubmed PY - 2021/4/7/medline KW - colon targeted drug delivery system KW - drug release KW - kinetics KW - mesalazine JF - Molecules (Basel, Switzerland) JO - Molecules VL - 25 IS - 23 N2 - Targeted drug delivery systems are a very convenient method of treating inflammatory bowel disease. The properties of pectin make this biopolymer a suitable drug carrier. These properties allow pectin to overcome the diverse environment of the digestive tract and deliver the drug to the large intestine. This investigation proposed bipolymeric formulations consisting of the natural polymer pectin and a synthetic polymer containing the drug 5-aminosalicylic acid. Pectin beads were prepared via ionotropic gelation involving the interaction between the hydrophilic gel and calcium ions. The obtained formulations consisted of natural polymer, 5-aminosalicylic acid (5-ASA) and one of the synthetic polymers, such as polyacrylic acid, polyvinylpyrrolidone, polyethylene glycol or aristoflex. The release of the drug was carried out employing a basket apparatus (USP 1). The acceptor fluid was pH = 7.4 buffer with added enzyme pectinase to reflect the colon environment. The amount of the released drug was determined using UV-Vis spectrophotometry at a wavelength of λ = 330 nm. The kinetics of the drug dissolution revealed that none of the employed models was appropriate to describe the release process. A kinetic analysis of the release profile during two release stages was carried out. The fastest drug release occurred during the first stage from a formulation containing pectin and polyethylene glycol. However, according to the applied kinetic models, the dissolution of 5-ASA was rather high in the formulation without the synthetic polymer during the second stage. Depending on the formulation, 68-77% of 5-ASA was released in an 8-hour time period. The FTIR and DSC results showed that there was no interaction between the drug and the polymers, but interactions between pectin and synthetic polymers were found. SN - 1420-3049 UR - https://www.unboundmedicine.com/medline/citation/33287276/Bipolymeric_Pectin_Millibeads_Doped_with_Functional_Polymers_as_Matrices_for_the_Controlled_and_Targeted_Release_of_Mesalazine_ DB - PRIME DP - Unbound Medicine ER -