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Article

Melt Amorphisation of Orlistat with Mesoporous Silica Using a Supercritical Carbon Dioxide: Effects of Pressure, Temperature, and Drug Loading Ratio and Comparison with Other Conventional Amorphisation Methods

1
College of Pharmacy, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Korea
2
Yonsei Institute of Pharmaceutical Sciences & College of Pharmacy, Yonsei University, 85 Songdogwahak-ro, Yeonsu-gu, Incheon 21983, Korea
3
Dong-A ST Co. Ltd., Giheung-gu, Yongin, Gyeonggi 446-905, Korea
*
Authors to whom correspondence should be addressed.
Both authors contributed equally to this work.
Current affiliation: Dong-A ST Co. Ltd., Giheung-gu, Yongin, Gyeonggi 446-905, Korea.
Pharmaceutics 2020, 12(4), 377; https://doi.org/10.3390/pharmaceutics12040377
Received: 26 March 2020 / Revised: 14 April 2020 / Accepted: 18 April 2020 / Published: 20 April 2020
(This article belongs to the Special Issue Advances in Oral and Buccal Drug Delivery)
The aim of this work was to develop an amorphous orlistat-loaded mesoporus silica formulation using the melt-amorphisation by supercritical fluid (MA-SCF) and to investigate the effects of pressure and temperature on the pharmaceutical properties of the developed formulation. In addition, the effect of orlistat mass ratio to the mesoporus silica was also evaluated. The carbon dioxide was used as a supercritical fluid, and Neusilin®UFL2 was selected as the mesoporous silica. For comparison with conventional amorphisation methods, orlistat formulations were also prepared by solvent evaporation and hot melt methods. Various pharmaceutical evaluations including differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, specific surface area, total pore volume, and content uniformity were performed to characterise the prepared orlistat formulation. The melting point depression and the solubility of orlistat in supercritical carbon dioxide (SC-CO2) were selected for the interpretation of evaluated results in relation to temperature and pressure. The total pore volume of the prepared orlistat-loaded mesoporus silica decreased with an increasing density of SC-CO2 to about 500 g/L at a constant temperature or pressure. From these results, it was suggested that increasing the density of SC-CO2 to about 500 g/L could result in the easier penetration of CO2 into molten orlistat and lower viscosity, hence facilitating the introduction and loading of orlistat into the pores of Neusilin®UFL2. However, when the density of SC-CO2 increased to more than 500 g/L, the total pore volume increased, and this may be due to the release out of orlistat from the pores of Neusilin®UFL2 by the increased orlistat solubility in SC-CO2. Interestingly, as the total pore volume decreased by the filling of the drug, the drug crystallinity decreased; hence, the dissolution rate increased. Furthermore, it was shown that the most desirable mass ratio of Neusilin®UFL2:orlistat for the amorphisation was 1:0.8 at an optimised supercritical condition of 318 K and 10 MPa. Compared with other amorphisation methods, only the sample prepared by the MA-SCF method was in pure amorphous state with the fastest dissolution rate. Therefore, it was concluded that the amorphous orlistat-loaded mesoporus silica prepared using MA-SCF under optimised conditions was more advantageous for enhancing the dissolution rate of orlistat than other conventional amorphisation methods. View Full-Text
Keywords: orlistat; mesoporous silica; supercritical carbon dioxide; melt-amorphisation; dissolution orlistat; mesoporous silica; supercritical carbon dioxide; melt-amorphisation; dissolution
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MDPI and ACS Style

Park, H.; Cha, K.-H.; Hong, S.H.; Abuzar, S.M.; Ha, E.-S.; Kim, J.-S.; Kim, M.-S.; Hwang, S.-J. Melt Amorphisation of Orlistat with Mesoporous Silica Using a Supercritical Carbon Dioxide: Effects of Pressure, Temperature, and Drug Loading Ratio and Comparison with Other Conventional Amorphisation Methods. Pharmaceutics 2020, 12, 377. https://doi.org/10.3390/pharmaceutics12040377

AMA Style

Park H, Cha K-H, Hong SH, Abuzar SM, Ha E-S, Kim J-S, Kim M-S, Hwang S-J. Melt Amorphisation of Orlistat with Mesoporous Silica Using a Supercritical Carbon Dioxide: Effects of Pressure, Temperature, and Drug Loading Ratio and Comparison with Other Conventional Amorphisation Methods. Pharmaceutics. 2020; 12(4):377. https://doi.org/10.3390/pharmaceutics12040377

Chicago/Turabian Style

Park, Heejun; Cha, Kwang-Ho; Hong, Seung H.; Abuzar, Sharif M.; Ha, Eun-Sol; Kim, Jeong-Soo; Kim, Min-Soo; Hwang, Sung-Joo. 2020. "Melt Amorphisation of Orlistat with Mesoporous Silica Using a Supercritical Carbon Dioxide: Effects of Pressure, Temperature, and Drug Loading Ratio and Comparison with Other Conventional Amorphisation Methods" Pharmaceutics 12, no. 4: 377. https://doi.org/10.3390/pharmaceutics12040377

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