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Titolo:
Preparation and characterization of insulin-loaded acrylic hydrogels containing absorption enhancers
Autore:
Uchida, T; Toida, Y; Sakakibara, S; Miyanaga, Y; Tanaka, H; Nishikata, M; Tazuya, K; Yasuda, N; Matsuyama, K;
Indirizzi:
Mukogawa Womens Univ, Fac Pharmaceut Sci, Nishinomiya, Hyogo 6638179, Japan Mukogawa Womens Univ Nishinomiya Hyogo Japan 6638179 Hyogo 6638179, Japan
Titolo Testata:
CHEMICAL & PHARMACEUTICAL BULLETIN
fascicolo: 10, volume: 49, anno: 2001,
pagine: 1261 - 1266
SICI:
0009-2363(200110)49:10<1261:PACOIA>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
RECTAL ABSORPTION; DRUG-DELIVERY; RATS;
Keywords:
hydrogel formulation; insulin; sodium salt of lauric acid; serum glucose level;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
16
Recensione:
Indirizzi per estratti:
Indirizzo: Uchida, T Mukogawa Womens Univ, Fac Pharmaceut Sci, 11-68 Koshien 9 Bancho, Nishinomiya, Hyogo 6638179, Japan Mukogawa Womens Univ 11-68 Koshien 9 Bancho Nishinomiya Hyogo Japan 6638179
Citazione:
T. Uchida et al., "Preparation and characterization of insulin-loaded acrylic hydrogels containing absorption enhancers", CHEM PHARM, 49(10), 2001, pp. 1261-1266

Abstract

The objectives of this study were to prepare insulin-loaded acrylic hydrogel formulations containing various absorption enhancers, to perform in vitro and in vivo characterization of these formulations, and to evaluate the factors which affecting insulin availability on rectal delivery of insulin using this hydrogel system. The acrylic block copolymer of methacrylic acid and methacrylate, Eudispert (R), was used to make the hydrogel formulations. As absorption enhancers, 2,6-di-O-methyl-beta -cyclodextrin (DM-beta -CyD), lauric acid (C12), or the sodium salt of C12 (C12Na), were incorporated into the hydrogels. In an in vitro release test, the release rate of insulin from the hydrogels decreased as the polymer concentration of the hydrogelincreased. The addition of C12Na to the hydrogel further increased the insulin release rate, which was greater at higher concentrations of the enhancer. A portion of the C12Na was found to remain bound to the acrylic polymerin dissolution medium. Serum insulin levels were determined at various time points after the administration of insulin solution or insulin-loaded (50units/kg body weight) Eudispert (R) hydrogels containing 5% (w/w) of C12, C12Na, or DM-beta -CyD to in situ loops in various regions of the rat intestine. The most effective enhancement of insulin release was observed with formulations containing C12Na. The bioavailability of insulin from the hydrogels was lower than that from the insulin solutions. Hydrogel formulations containing 7% or 10% Eudispert (R) remained in the rectum for 5 h after rectal administration. However, the 5% (w/w) C12Na solution stained with Evan's-blue had diffused out and the dye had reached the upper intestinal tract within 2 h. Finally, the rectal administration of insulin-loaded hydrogels,containing 4%, 7%, or 10% (w/w) Eudispert (R) and 5% (w/w) of enhancer (C12, C12Na, or DM-beta -CyD) to normal rats was shown to decrease serum glucose concentrations. The greatest effect was found with insulin-loaded 7% (Eudispert (R)) hydrogel containing C12Na which having considerable large insulin release rate and bioadhesive characteristics.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 05:53:24