Evaluation of mesoporous TCPSi, MCM-41, SBA-15, and TUD-1 materials as API carriers for oral drug delivery.
The feasibility of four mesoporous materials composed of biocompatible Si (TCPSi) or SiO(2) (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.
Heikkilä
T
T
Laboratory of Industrial Physics, Department of Physics, University of Turku, Turku, Finland.
Salonen
J
J
Tuura
J
J
Kumar
N
N
Salmi
T
T
Murzin
D Yu
DY
Hamdy
M S
MS
Mul
G
G
Laitinen
L
L
Kaukonen
A M
AM
Hirvonen
J
J
Lehto
V-P
VP
D000284:Administration, Oral; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D007052:Ibuprofen / Q000008:administration & dosage / Q000737:chemistry; D010539:Permeability; D016062:Porosity; D012825:Silicon / Q000737:chemistry*; D012822:Silicon Dioxide / Q000737:chemistry*; D012995:Solubility; D014961:X-Ray Diffraction
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; C509968:MCM-41; C509969:SBA-15; D012822:Silicon Dioxide; D007052:Ibuprofen; D012825:Silicon