Review: Mesoporous Silica Formulation in Biopharmaceutical Classification System (BCS) Class II Drug Development
Abstract
About 40% of approved drugs and nearly 90% of drug candidates have low aqueous solubility which limits their bioavailability resulting in suboptimal pharmacological activity. According to the Biopharmaceutical Classification System (BCS), drugs with low solubility and high permeability are categorized as BCS Class II, where the dissolution rate becomes a key factor in gastrointestinal absorption. One approach to increasing its solubility is the formation of an amorphous state, which lowers lattice energy and enhances dissolution. However, the amorphous form tends to be unstable and prone to recrystallization. Mesoporous silica has been developed as a drug delivery system capable of maintaining the stability of the amorphous form through molecular interactions with silanol groups and the nano-confinement effect that suppresses crystal growth. With a high surface area and tunable pore structure, mesoporous silica enhances the dissolution rate and bioavailability of BCS Class II drugs, ultimately contributing to improved pharmacological activity. This review summarizes the development of mesoporous silica formulations in drug delivery systems for BCS Class II drugs to enhance their pharmacological efficacy.
Full Text:
PDFReferences
Alany R. Oral dosage forms and drug delivery systems: tablets, oral films, liquid dosage forms, oral bioavailability enhancement. Vol. 22, Pharmaceutical Development and Technology. 2017;22(2):137.
Kumari L, Choudhari Y, Patel P, Gupta G Das, Singh D, Rosenholm JM, et al. Advancement in Solubilization Approaches: A Step towards Bioavailability Enhancement of Poorly Soluble Drugs. Life. 2023;13(5):1099.
Wang JX, Zhang ZB, Le Y, Zhao H, Chen JF. A novel strategy to produce highly stable and transparent aqueous “nanosolutions” of water-insoluble drug molecules. Nanotechnology. 2011;22(30):86-89.
Jermain S V, Brough C, Williams RO. Amorphous solid dispersions and nanocrystal technologies for poorly water-soluble drug delivery – An update. Int J Pharm. 2018 Jan;535(1–2):379–92.
Dahan A, Miller JM, Amidon GL. Prediction of solubility and permeability class membership: Provisional BCS classification of the world’s top oral drugs. AAPS Journal. 2009;11(4):740–6.
Bhalani D V., Nutan B, Kumar A, Singh Chandel AK. Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics. Biomedicines.
Karagianni A, Kachrimanis K, Nikolakakis I. Co-amorphous solid dispersions for solubility and absorption improvement of drugs: Composition, preparation, characterization and formulations for oral delivery. Pharmaceutics. 2018;10(3):98.
Wang H, Zhao P, Ma R, Jia J, Fu Q. Drug–drug co-amorphous systems: An emerging formulation strategy for poorly water-soluble drugs. Drug Discov Today. 2024 Feb 1;29(2):103883.
Kim DH, Kim YW, Tin YY, Soe MTP, Ko BH, Park SJ, et al. Recent technologies for amorphization of poorly water-soluble drugs. Pharmaceutics. 2021;13(8):1318.
Kanaujia P, Poovizhi P, Ng WK, Tan RBH. Amorphous formulations for dissolution and bioavailability enhancement of poorly soluble APIs. Powder
Technol. 2015;285:2–15.
Ma X, Williams RO. Characterization of amorphous solid dispersions: An update. J Drug Deliv Sci Technol. 2019;50(2019):113–24.
Minqian Luo, Weili Heng, Juan Dai, Yuanfeng Wei, Yuan Gao, Jianjun Zhang. Crystallization of Amorphous Drugs and Inhibiting Strategies. Prog Chem. 2021;33(11):2116–27.
Becelaere J, Van Den Broeck E, Schoolaert E, Vanhoorne V, Van Guyse JFR, Vergaelen M, et al. Stable amorphous solid dispersion of flubendazole with high loading via electrospinning. J Control Release. 2022;351:123–36.
Chavan RB, Thipparaboina R, Kumar D, Shastri NR. Co amorphous systems: A product development perspective. Int J Pharm. 2016;515(1–2):403–15.
Yan J, Siwakoti P, Shaw S, Bose S, Kokil G, Kumeria T. Porous silicon and silica carriers for delivery of peptide therapeutics. Drug Deliv Transl Res. 2024;14(12):3549–67.
Desai D, Åkerfelt M, Prabhakar N, Toriseva M, Näreoja T, Zhang J, et al. Factors Affecting Intracellular Delivery and Release of Hydrophilic Versus Hydrophobic Cargo from Mesoporous Silica Nanoparticles on 2D and 3D Cell Cultures. Pharmaceutics. 2018;10(4):237.
Narayan R, Nayak UY, Raichur AM, Garg S. Mesoporous Silica Nanoparticles: A Comprehensive Review on Synthesis and Recent Advances. Pharmaceutics. 2018;10(3):118.
Senapati S, Mahanta AK, Kumar S, Maiti P. Controlled drug delivery vehicles for cancer treatment and their performance. Signal transduction and targeted therapy. 2018;3(1):7.
Prajapati RU, Bhattacharyya S. A Comprehensive Review on Mesoporous Silica Nanoparticles: A Novel Pharmaceutical Aid for Drug Delivery. Indian Journal of Pharmaceutical Sciences. 2023;85(5).
Taki H, Ishida M, Otsuka M. One-step preparation of sustained-release ASDs using mesoporous spherical silica.
Budiman A, Anastasya G, Handini AL, Lestari IN, Subra L, Aulifa DL. Characterization of Drug with Good Glass-Forming Ability Loaded Mesoporous Silica Nanoparticles and Its Impact Toward in vitro and in vivo Studies. International Journal of Nanomedicine. 2024;19:2199-25.
Seljak KB, Kocbek P, Gašperlin M. Mesoporous silica nanoparticles as delivery carriers: An overview of drug loading techniques. J Drug Deliv Sci Technol. 2020;59:101906.
Trzeciak K, Chotera‐ouda A, Bak‐sypien II, Potrzebowski MJ. Mesoporous Silica Particles as Drug Delivery Systems—The State of the Art in Loading Methods and the Recent Progress in Analytical Techniques for Monitoring These Processes. Pharmaceutics. 2021;13(7):950.
Khalbas AH, Albayati TM, Ali NS, Salih IK. Drug loading methods and kinetic release models using of mesoporous silica nanoparticles as a drug delivery system: A review. South African J Chem Eng. 2024;50:261–80.
Subramaniam S, Thomas N, Gustafsson H, Jambhrunkar M, Kidd SP, Prestidge CA. Rifampicin-Loaded Mesoporous Silica Nanoparticles for the Treatment of Intracellular Infections. Antibiotics. 2019;8(2):39.
Ferreira NH, Ribeiro AB, Rinaldi-Neto F, Fernandes FS, do Nascimento
S, Braz WR, et al. Anti-Melanoma Activity of Indomethacin Incorporated into Mesoporous Silica Nanoparticles. Pharmaceutical Research. 2020;37(172):1-11.
Wang Y, Ke J, Gou K, Guo Y, Xu X, Li S, et al. Amino functionalized mesoporous silica with twisted rod-like shapes: Synthetic design, in vitro and in vivo evaluation for ibuprofen delivery. Microporous Mesoporous Mater. 2020;294:109896.
Masood A, Maheen S, Khan HU, Shafqat SS, Irshad M, Aslam I, et al. Pharmaco-Technical Evaluation of Statistically Formulated and Optimized Dual Drug-Loaded Silica Nanoparticles for Improved Antifungal Efficacy and Wound Healing. ACS omega. 2021;6(12):8210–8225.
Abd-Elrahman AA, El Nabarawi MA, Hassan DH, Taha AA. Ketoprofen mesoporous silica nanoparticles SBA-15 hard gelatin capsules: preparation and in vitro/in vivo characterization. Drug Deliv. 2016;23(9):3387–98.
Chaudhary Z, Subramaniam S, Khan GM, Abeer MM, Qu Z, Janjua T, et al. Encapsulation and Controlled Release of Resveratrol Within Functionalized Mesoporous Silica Nanoparticles for Prostate Cancer Therapy. Frontiers in bioengineering and biotechnology. 2019;7:225.
Yang G, Li Z, Wu FH, Chen MY, Wang R, Zhu H, et al. Improving Solubility and Bioavailability of Breviscapine with Mesoporous Silica Nanoparticles Prepared Using Ultrasound-Assisted Solution-Enhanced Dispersion by Supercritical Fluids Method. Int J Nanomedicine. 2020;15:1661–75.
Li J, Wang H, Yang B, Xu L, Zheng N, Chen H, et al. Control-release microcapsule of famotidine loaded biomimetic synthesized mesoporous
silica nanoparticles: Controlled release effect and enhanced stomach adhesion in vitro. Mater Sci Eng C. 2016;58:273–7.
Díaz-García D, Ferrer-Donato Á, Méndez-Arriaga JM, Cabrera-Pinto M, Díaz-Sánchez M, Prashar S, et al. Design of Mesoporous Silica Nanoparticles for the Treatment of Amyotrophic Lateral Sclerosis (ALS) with a Therapeutic Cocktail Based on Leptin and Pioglitazone. ACS Biomater Sci Eng. 2022;8(11):4838–49.
Wang Y, Sun L, Jiang T, Zhang J, Zhang C, Sun C, et al. The investigation of MCM-48-type and MCM-41-type mesoporous silica as oral solid dispersion carriers for water insoluble cilostazol. Drug Dev Ind Pharm. 2014;40(6):819–28.
Pardhi V, Chavan RB, Thipparaboina R, Thatikonda S, Naidu VGM, Shastri NR. Preparation, characterization, and cytotoxicity studies of niclosamide loaded mesoporous drug delivery systems. Int J Pharm. 2017;528(1–2):202–14.
Musallam AA, Mahdy MA, Elnahas HM, Aldeeb RA. Optimization of mirtazapine loaded into mesoporous silica nanostructures via Box-Behnken design: in-vitro characterization and in-vivo assessment. Drug Deliv. 2022;29(1):1582–94.
Mahajan M, Rajput S. Development of Mesoporous Silica Nanoparticles of Ritonavir With Enhanced Bioavailability Potential: Formulation Optimization, in-Vitro and in-Vivo Evaluation. Int J Pharm Sci Res. 2018;9(10):4127.
Velho MC, Funk NL, Deon M, Benvenutti EV, Buchner S, Hinrichs R, et al. Ivermectin-Loaded Mesoporous Silica and Polymeric Nanocapsules: Impact on Drug
Loading, In Vitro Solubility Enhancement, and Release Performance. Pharmaceutics. 2024;16(3).
Voycheva CT, Tzankov B, Tzankova DG, Avramova KI, Yoncheva KP. Formulation of tablets containing glimepiride-loaded mesoporous silica particles. Indian J Pharm Sci. 2019;81(3):483–8.
Li Z, Zhang Y, Feng N. Mesoporous silica nanoparticles: synthesis, classification, drug loading, pharmacokinetics, biocompatibility, and application in drug delivery. Expert Opin Drug Deliv. 2019;16(3):219–37.
Tella JO, Adekoya JA, Ajanaku KO. Mesoporous silica nanocarriers as drug delivery systems for anti-tubercular agents: A review. R Soc Open Sci. 2022;9(6):1-26.
Kankala RK, Han YH, Xia HY, Wang S Bin, Chen AZ. Nanoarchitectured prototypes of mesoporous silica nanoparticles for innovative biomedical applications. J Nanobiotechnology. 2022;20(1):1–67.
Fedorowicz Z, van Zuuren EJ, Hu N. Histamine H2-receptor antagonists for urticaria. Cochrane Database of Systematic Reviews. 2012;(3).
Richter B, Bandeira-Echtler E, Bergerhoff K, Clar C, Ebrahim SH. Pioglitazone for type 2 diabetes mellitus. Cochrane Database of Systematic Reviews. 2006;(4).
Jia Y, Zhang H, Yang S, Xi Z, Tang T, Yin R, et al. Electrospun PLGA Membrane Incorporated With andrographolide-loaded Mesoporous Silica Nanoparticles for Sustained Antibacterial Wound Dressing. Nanomedicine. 2018;13(22):2881–99.
Refbacks
- There are currently no refbacks.
