Abstract
Porous silicon (PSi) is an innovative inorganic material that has been recently developed for various drug delivery systems. For example, hydrophilic and hydrophobic PSi microparticles have been utilized to improve the dissolution rate of poorly soluble drugs and to sustain peptide delivery. Previously, the well-plate method has been demonstrated to be a suitable in vitro dissolution method for hydrophilic PSi particles but it was not applicable to poorly wetting hydrophobic thermally hydrocarbonized PSi (THCPSi) particles. In this work, three different in vitro dissolution techniques, namely centrifuge, USP Apparatus 1 (basket) and well-plate methods were compared by using hydrophilic thermally carbonized PSi (TCPSi) microparticles loaded with poorly soluble ibuprofen or freely soluble antipyrine. All the methods showed a fast and complete or nearly complete release of both model compounds from the TCPSi microparticles indicating that all methods described in vitro dissolution equally. Based on these results, the centrifuge method was chosen to study the release of a peptide (ghrelin antagonist) from the THCPSi microparticles since it requires small sample amounts and achieves good particle suspendability. Sustained peptide release from the THCPSi microparticles was observed, which is in agreement with an earlier in vivo study. In conclusion, the centrifuge method was demonstrated to be a suitable tool for the evaluation of drug release from hydrophobic THCPSi particles, and the sustained peptide release from THCPSi microparticles was detected.
Highlights
Porous silicon (PSi) is an inorganic mesoporous material that has been developed in recent years for particulate drug delivery systems and it is fabricated from silicon wafers by electrochemical etching of silicon in hydrofluoric acid [1,2]
USP Apparatus 1, centrifuge and well plate methods were compared by using hydrophilic
Virtually no crystallized (
Summary
Porous silicon (PSi) is an inorganic mesoporous material that has been developed in recent years for particulate drug delivery systems and it is fabricated from silicon wafers by electrochemical etching of silicon in hydrofluoric acid [1,2]. Unlike the situation for tablets or capsules, there is no gold standard for assessing release from particulate drug delivery systems, instead, many different in vitro drug release tests have been developed and the field is still evolving. The commonly used methods for testing of drug release from particulate drug delivery systems can be divided into three classes: 1) sample and separate; 2) dialysis; and 3) continuous flow methods [10,11]. Well-plates with cell culture inserts have been commonly used to study drug release from hydrophilic thermally oxidized (TOPSi) or thermally carbonized (TCPSi) PSi microparticles [3,4,5]. The well-plate method is not suitable for hydrophobic THCPSi microparticles as the wettability of these particles is poor and they are not homogenously dispersed in the dissolution medium but float on the surface [12]
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