Evaluation of mesoporous TCPSi, MCM-41, SBA-15, and TUD-1 materials as API carriers for oral drug delivery

被引:156
作者
Heikkila, T.
Salonen, J.
Tuura, J.
Kumar, N.
Salmi, T.
Murzin, D. Yu.
Hamdy, M. S.
Mul, G.
Laitinen, L.
Kaukonen, A. M.
Hirvonen, J.
Lehto, V.-P. [1 ]
机构
[1] Univ Turku, Dept Phys, Lab Ind Phys, FI-20014 Turku, Finland
[2] Univ Helsinki, Fac Pharm, Div Pharmaceut Technol, Helsinki, Finland
[3] Univ Helsinki, Drug Discovery & Dev Technol Ctr, Helsinki, Finland
[4] Delft Univ Technol, Delft, Netherlands
[5] Abo Akad Univ, Proc Chem Ctr, Lab Ind Chem, Turku, Finland
[6] Grad Sch Mat Res, Turku, Finland
关键词
dissolution enhancement; drug delivery; drug loading; drug release; mesoporous materials;
D O I
10.1080/10717540601098823
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The feasibility of four mesoporous materials composed of biocompatible Si (TCPSi) or SiO, (MCM-41, SBA-15, and TUD-1) were evaluated for oral drug delivery applications. The main focus was to study the effect of the materials different pore systems (unidirectional/2D/3D) and their pore diameters, pore size distributions, pore volumes on the maximal drug load capacity, and release profiles of a loaded active pharmaceutical ingredient. Ibuprofen was used as the model drug. The total pore volume of the mesoporous solid was the main factor limiting the maximum drug load capacity, with SBA-15 reaching a very high drug load of 1:1 in weight due to its high pore volume. Dissolution experiments were performed in HBSS buffers of pH 5.5, 6.8, and 7.4 to mimic the conditions in the small intestine. At pH 5.5 the dissolution rate of ibuprofen released from the mesoporous carriers was significantly faster compared with the standard bulk ibuprofen (86-63% versus 25 % released at 45 min), with the fastest release observed from the 3D pore network of TUD-1 carrier. The utilization of mesoporous carriers diminished the pH dependency of ibuprofen dissolution (pK(a) = 4.42), providing an interesting prospect for the formulation of poorly soluble drug compounds.
引用
收藏
页码:337 / 347
页数:11
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