CHARACTERIZATION OF DRUGS ENCAPSULATED INTO MESOPOROUS SILICA
DOI:
https://doi.org/10.22159/ijap.2019v11i6.35431Keywords:
Poorly water-soluble drug, Mesoporous silica, Amorphous, Dissolution enhancementAbstract
Solubility of the drug has a strong influence to achieve higher bioavailability of the drug in systemic circulation. More than 70% NCEs (new chemical entities) are hydrophobic, and practically difficult into solid formulation due to their poor water solubility. Mesoporous silicas (MSP) have been used for drug delivery system, especially for poorly water-soluble drugs. Encapsulation and interaction of drugs in MSP can enhance the delivery and maintain the stability of the drug. However, the characterization of the drug in MSP is necessary to confirm its molecular state. In this review, we present an overview of reports related to the characterization of drug encapsulated into MSP. Encapsulation of drugs in MSP can prevent recrystallization of drugs due to its inhibition of crystal nucleation. A porous material in MSP can maintain the drug in a physically stable amorphous state. The preventing of drug crystallization in MSP can enhance the solubility and the dissolution rate of drug. Therefore, in this work, attempts have been made to understand the molecular state of the drug in MSP. The physicochemical characterization of drug by transmission electron microscopy (TEM), scanning electron microscope (SEM), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), powder x-ray diffraction (PXRD) and thermogravimetric analysis (TGA) were discussed. The effect of solvent and methods of drug loading and the effect of the shape of MSP on release profiles are also presented. Overall, this review provides information about the characterization of drug encapsulated into MSP which will be useful in pharmaceutical formulation development.
Downloads
References
Skorupska E, Jeziorna A, Potrzebowski MJ. Thermal solvent-free method of loading of pharmaceutical cocrystals into the pores of silica particles: a case of naproxen/picolinamide cocrystal. J Phys Chem C 2016;120:13169-80.
Edward KH, Li D. Drug Like Properties: Concept, Structure, Design and Methods, from ADME to Toxicity Optimization; Solubility Elsevier: New York, NY, USA; 2008. p. 56.
Sathisaran I, Dalvi S. Engineering cocrystals of poorly water-soluble drugs to enhance dissolution in an aqueous medium. Pharmaceutics 2018;10:108.
Skorupska E, Paluch P, Jeziorna A, Potrzebowski MJ. NMR study of BA/FBA cocrystal confined within mesoporous silica nanoparticles employing thermal solid phase transformation. J Phys Chem C 2015;119:8652-61.
Mellaerts R, Jammaer JA, Van Speybroeck M, Chen H, Humbeeck JV, Augustijns P, et al. Physical state of poorly water-soluble therapeutic molecules loaded into SBA-15 ordered mesoporous silica carriers: a case study with itraconazole and ibuprofen. Langmuir 2008;24:8651-9.
Yamamoto K, Kojima T, Karashima M, Ikeda Y. Physicochemical evaluation and developability assessment of co-amorphouses of low soluble drugs and comparison to the co-crystals. Chem Pharm Bull 2016;64:1739-46.
Azad M, Moreno J, Dave R. Stable and fast-dissolving amorphous drug composites preparation via impregnation of Neusilin® UFL2. J Pharm Sci 2018;107:170-82.
Wang S. Ordered mesoporous materials for drug delivery. Micropor Mesopor Mat 2009;117:1-9.
Wang Y, Zhao Q, Han N, Bai L, Li J, Liu J, et al. Mesoporous silica nanoparticles in drug delivery and biomedical applications. Nanomed Nanotechnol 2015;11:313-27.
Slowing II, Trewyn BG, Giri S, Lin VY. Mesoporous silica nanoparticles for drug delivery and biosensing applications. Adv Func Mat 2007;17:1225-36.
Kinnari P, Makila E, Heikkila T, Salonen J, Hirvonen J, Santos HA. Comparison of mesoporous silicon and non-ordered mesoporous silica materials as drug carriers for itraconazole. Int J Pharm 2011;414:148-56.
Ali KH, Ansari MM, Shah FA, Din FU, Basit MA, Kim JK, et al. Enhanced dissolution of valsartan-vanillin binary co-amorphous system loaded in mesoporous silica particles. J Microencapsul 2019;36:1-11.
Bi Y, Xiao D, Ren S, Bi S, Wang J, Li F. The binary system of ibuprofen-nicotinamide under nanoscale confinement: from cocrystal to coamorphous state. J Pharm Sci 2017;106:3150-5.
Van Speybroeck M, Mellaerts R, Mols R, Do Thi T, Martens JA, Van Humbeeck J, et al. Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica. Eur J Pharm Sci 2010;41:623-30.
Shen SC, Ng WK, Chia L, Dong YC, Tan RB. Stabilized amorphous state of ibuprofen by co‐spray drying with mesoporous SBA‐15 to enhance dissolution properties. J Pharm Sci 2010;99:1997-2007.
Mellaerts R, Mols R, Jammaer JA, Aerts CA, Annaert P, Van Humbeeck J, et al. Increasing the oral bioavailability of the poorly water-soluble drug itraconazole with ordered mesoporous silica. Eur J Pharm Biopharm 2008;69:223-30.
Mellaerts R, Aerts CA, Van Humbeeck J, Augustijns P, Van den Mooter G, Martens JA. Enhanced release of itraconazole from ordered mesoporous SBA-15 silica materials. Chem Comm 2007;13:1375-7.
Kinnari P, Makila E, Heikkila T, Salonen J, Hirvonen J, Santos HA. Comparison of mesoporous silicon and non-ordered mesoporous silica materials as drug carriers for itraconazole. Int J Pharm 2011;414:148-56.
Van Speybroeck M, Mellaerts R, Thi TD, Martens JA, Van Humbeeck J, Annaert P, et al. Preventing release in the acidic environment of the stomach via occlusion in ordered mesoporous silica enhances the absorption of poorly soluble weakly acidic drugs. J Pharm Sci 2011;100:4864-76.
Tozuka Y, Wongmekiat A, Kimura K, Moribe K, Yamamura S, Yamamoto K. Effect of pore size of FSM-16 on the entrapment of flurbiprofen in mesoporous structures. Chem Pharm Bull 2005;53:974-7.
Zhao P, Wang L, Sun C, Jiang T, Zhang J, Zhang Q, et al. Uniform mesoporous carbon as a carrier for poorly water soluble drug and its cytotoxicity study. Eur J Pharm Biopharm 2012;80:535-43.
Jambhrunkar S, Karmakar S, Popat A, Yu M, Yu C. Mesoporous silica nanoparticles enhance the cytotoxicity of curcumin. RSC Adv 2014;4:709-12.
Zhang Y, Zhi Z, Jiang T, Zhang J, Wang Z, Wang S. Spherical mesoporous silica nanoparticles for loading and release of the poorly water-soluble drug telmisartan. J Controlled Release 2010;145:257-63.
Ambrogi V, Perioli L, Marmottini F, Giovagnoli S, Esposito M, Rossi C. Improvement of dissolution rate of piroxicam by inclusion into MCM-41 mesoporous silicate. Eur J Pharm Sci 2007;32:216-22.
Xu W, Riikonen J, Lehto VP. Mesoporous systems for poorly soluble drugs. Int J Pharm 2013;453:181-97.
Lai J, Lin W, Scholes P, Li M. Investigating the effects of loading factors on the in vitro pharmaceutical performance of mesoporous materials as drug carriers for ibuprofen. Materials 2017;10:150.
Hu L, Sun C, Song A, Chang D, Zheng X, Gao Y, et al. Alginate encapsulated mesoporous silica nanospheres as a sustained drug delivery system for the poorly water-soluble drug indomethacin. Asian J Pharm Sci 2014;9:183-90.
Kiwilsza A, Milanowski B, Drużbicki K, Coy LE, Grzeszkowiak M, Jarek M, et al. Mesoporous drug carrier systems for an enhanced delivery rate of poorly water-soluble drug: nimodipine. J Porous Mat 2015;22:817-29.
Meka A, Jenkins L, Davalos Salas M, Pujara N, Wong K, Kumeria T, et al. Enhanced solubility, permeability and anticancer activity of vorinostat using tailored mesoporous silica nanoparticles. Pharmaceutics 2018;10:283.
Nafisi S, Samadi N, Houshiar M, Maibach HI. Mesoporous silica nanoparticles for enhanced lidocaine skin delivery. Int J Pharm 2018;550:325-32.
Heikkila T, Salonen J, Tuura J, Kumar N, Salmi T, Murzin DY, et al. Evaluation of mesoporous TCPSi, MCM-41, SBA-15, and TUD-1 materials as API carriers for oral drug delivery. Drug Delivery 2007;14:337–47.
Hong S, Shen S, Tan DCT, Ng WK, Liu X, Chia LS, et al. High drug load, stable, manufacturable and bioavailable fenofibrate formulations in mesoporous silica: a comparison of spray drying versus solvent impregnation methods. Drug Delivery 2016;23:316-27.
Salonen J, Laitinen L, Kaukonen AM, Tuura J, Bjorkqvist M, Heikkila T, et al. Mesoporous silicon microparticles for oral drug delivery: loading and release of five model drugs. J Controlled Release 2005;108:362–74.
Soltys M, Kovacik P, Dammer O, Beranek J, Stepanek F. Effect of solvent selection on drug loading and amorphization in mesoporous silica particles. Int J Pharm 2019;555:19-27.
Makila E, Kivela H, Shrestha N, Correia A, Kaasalainen M, Kukk E, et al. Influence of surface chemistry on ibuprofen adsorption and confinement in mesoporous silicon microparticles. Langmuir 2016;32:13020-9.
Hillerstrom A, Andersson M, Samuelsson J, van Stam J. Solvent strategies for loading and release in mesoporous silica. Colloid Interfac Sci 2014;3:5-8.
Sanjay C, Ghate VM, Lewis SA. Mesoporous silica particles for dermal drug delivery: a review. Int J Appl Pharm 2018;10:23-6.
Banerjee A, Qi JP, Gogoi R, Wong J, Mitragotri S. Role of nanoparticle size, shape, and surface chemistry in oral drug delivery. J Controlled Release 2016;238:176–85.
Landry CC, Tolbert SH, Gallis KW, Monnier A, Stucky GD, Norby F, et al. Phase transformations in mesostructured silica/surfactant composites. Mechanisms for change and applications to materials synthesis. Chem Mat 2001;13:1600–8.
Sharmiladevi S, Priya AS, Sujitha M. Synthesis of mesoporous silica nanoparticles and drug loading for gram-positive and gram-negative bacteria International. J Pharm Pharm Sci 2016;8:196-201.
Zhang W, Zheng N, Chen L, Xie L, Cui M, Li S, et al. Effect of shape on mesoporous silica nanoparticles for oral delivery of indomethacin. Pharmaceutics 2019;11:4.