Characterization of Drug with Good Glass-Forming Ability Loaded Mesoporous Silica Nanoparticles and Its Impact Toward in vitro and in vivo Studies

Abstract

Arif Budiman,1 Gracia Anastasya,1 Annisa Luthfiyah Handini,1 Ira Novianty Lestari,2 Laila Subra,3 Diah Lia Aulifa2 1Department of Pharmaceutics and Pharmaceutical Technology, Universitas Padjadjaran, Bandung, Indonesia; 2Department of Pharmaceutical Analysis and Medicinal Chemistry, Universitas Padjadjaran, Bandung, Indonesia; 3Department of Pharmacy, Universiti Geomatika Malaysia, Kuala Lumpur, MalaysiaCorrespondence: Diah Lia Aulifa, Department of Pharmaceutical Analysis and Medicinal Chemistry, Universitas Padjadjaran, Jl, Raya Bandung-Sumedang Km. 21, Bandung, 45363, Indonesia, Email [email protected]: Solid oral dosage forms are mostly preferred in pharmaceutical formulation development due to patient convenience, ease of product handling, high throughput, low manufacturing costs, with good physical and chemical stability. However, 70% of drug candidates have poor water solubility leading to compromised bioavailability. This phenomenon occurs because drug molecules are often absorbed after dissolving in gastrointestinal fluid. To address this limitation, delivery systems designed to improve the pharmacokinetics of drug molecules are needed to allow controlled release and target-specific delivery. Among various strategies, amorphous formulations show significantly high potential, particularly for molecules with solubility-limited dissolution rates. The ease of drug molecules to amorphized is known as their glass-forming ability (GFA). Specifically, drug molecules categorized into class III based on the Taylor classification have a low recrystallization tendency and high GFA after cooling, with substantial “glass stability” when heated. In the last decades, the application of mesoporous silica nanoparticles (MSNs) as drug delivery systems (DDS) has gained significant attention in various investigations and the pharmaceutical industry. This is attributed to the unique physicochemical properties of MSNs, including high loading capacity, recrystallization inhibition, excellent biocompatibility, and easy functionalization. Therefore, this study aimed to discuss the current state of good glass former drug loaded mesoporous silica and shows its impact on the pharmaceutical properties including dissolution and physical stability, along with in vivo study. The results show the importance of determining whether mesoporous structures are needed in amorphous formulations to improve the pharmaceutical properties of drug with a favorable GFA. Keywords: mesoporous silica nanoparticles, good glass-forming ability, characterization, dissolution, in vivo study

Keywords

• mesoporous silica nanoparticles
• good glass-forming ability
• characterization
• dissolution
• in vivo study.