Eudragit® and hydrotalcite-like anionic clay composite system for diclofenac colonic delivery

被引:45
作者
Ambrogi, V. [1 ]
Perioli, L. [2 ]
Ricci, M. [1 ]
Pulcini, L. [1 ]
Nocchetti, M. [2 ]
Giovagnoli, S. [1 ]
Rossi, C. [1 ]
机构
[1] Univ Perugia, Dipartimento Chim & Tecnol Farm, I-06123 Perugia, Italy
[2] Univ Perugia, Dipartimento Chim, I-06123 Perugia, Italy
关键词
hydrotalcite-like anionic clays; diclofenac; composite system; colonic delivery; Eudragite;
D O I
10.1016/j.micromeso.2008.02.014
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
In this paper, the microencapsulation of the MgAl-hydrotalcite (HTlc) and diclofenac (DIK) intercalation product (HT]c-DIK) was realized in order to obtain a composite system for colonic drug delivery. Eudragite (R) S or Eudragit (R) L were used as polymers for preparation of microparticles (MPs). MPs were prepared by using a properly modified oil-in-oil solvent evaporation method. A 1:5 or 1:10 w/w HTlc-DIK/polymer ratios were employed. An experimental design was applied in order to assess the preparation variable effects oil the qualitative MP appearance. Improved MP preparations were achieved when 7-13 ml of acetone-ethanol solution was employed at both HTlc-DIK/polymer ratios. The MPs were tested for in vitro drug release. DIK release from Eudragite L MPs at pH 6.8 reached 26-35X, within 25-30 min at both HTlc-DIK/polymer ratios and no further increase was observed when the pH was shifted to 7.5. DIK release from Eudragite S MPs at pH 7.5 reached for both ratios 70%, after 6-8 h. The obtained results showed that hydrotalcite intercalation compound call be microencapsulated without missing the intercalated compound and the resulted composite MPs showed good characteristics. Besides HTlc-DIK/Eudragit (R) S MPs possess improved features with respect to HTlc-DIK/Eudragit (R) L MPs. For this reason, HTlc-DIK/Eudragit (R) S MPs could be promising for drug delivery either to the distal part of small intestine or to the colon. (c) 2008 Elsevier Inc. All rights reserved.
引用
收藏
页码:405 / 415
页数:11
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