Amorphous solid dispersions stabilized by one or more polymer(s) have been widely used for delivering amorphous drugs with poor water solubilities, and they have gained great market success. Polymer selection is important for preparing robust amorphous solid dispersions, and considerations should be given as to how the critical attributes of a polymer can enhance the physical stability, and the in vitro and in vivo performances of a drug. This article provides a comprehensive overview for recent developments in the understanding the role of polymers in amorphous solid dispersions from the aspects of nucleation, crystal growth, overall crystallization, miscibility, phase separation, dissolution, and supersaturation. The critical properties of polymers affecting the physical stability and the in vitro performance of amorphous solid dispersions are also highlighted. Moreover, a perspective regarding the current research gaps and novel research directions for better understanding the role of the polymer is provided. This review will provide guidance for the rational design of polymer-based amorphous pharmaceutical solids with desired physicochemical properties from the perspective of physical stability and in vitro performance.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9413000 | PMC |
| http://dx.doi.org/10.3390/pharmaceutics14081747 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Developing Soluplus®-Based Microparticle Amorphous Solid Dispersions with High Drug Loading for Enhanced Celecoxib Dissolution via Electrospraying.
AAPS PharmSciTech
January 2025
Laboratory of Advanced Theranostic Materials and Technology, Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo, 315201, China.
Amorphous solid dispersion (ASD) is one of the most studied strategies for improving the dissolution performance of poorly water-soluble drugs, but ASDs often have low drug loadings, thereby necessitating larger dosage sizes. This study intended to create Soluplus® (SOL)-based microparticle ASDs with high drug loading (up to 60 w/w%) and long-term stability (at least 16 months) using electrospraying to enhance the dissolution of poorly water-soluble celecoxib (CEL). X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses showed that the electrosprayed SOL-CEL microparticles were amorphous, and Fourier transform infrared spectroscopy (FTIR) data indicated the presence of hydrogen bonding between SOL and CEL in the microparticles, which helped stabilize the ASDs.
View Article and Find Full Text PDFAssessing the Impacts of Drug Loading and Polymer Type on Dissolution Behavior and Diffusive Flux of GDC-6893 Amorphous Solid Dispersions.
J Pharm Sci
January 2025
Department of Synthetic Molecule Pharmaceutical Sciences, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address:
It is desirable but remains challenging to develop high drug load amorphous solid dispersions (ASDs) without compromising their quality attributes and bio-performance. In this work, we investigated the impacts of formulation variables, such as drug loading (DL) and polymer type, on dissolution behavior, diffusive flux, and in vitro drug absorption of ASDs of a high T compound, GDC-6893. ASDs with two polymers (HPMCAS and PVPVA) and various DLs (20 - 80%) were produced by spray drying and their drug-polymer miscibility was evaluated using solid-state nuclear magnetic resonance (ssNMR).
View Article and Find Full Text PDFPhysical Isolation Strategy in Multi-Layer Self-Nanoemulsifying Pellets: Improving Dissolution and Drug Loading Efficiency of Ramipril.
J Pharm Sci
January 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, POBOX-2457, Riyadh 11451, Kingdom of Saudi Arabia; Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Kingdom of Saudi Arabia. Electronic address:
Background And Purpose: Liquid self-nanoemulsifying drug delivery systems (SNEDDS) face challenges related to stability, handling, and storage. In particular, lipophilic and unstable drugs, such as ramipril (RMP) and thymoquinone (THQ), face challenges in oral administration due to poor aqueous solubility and chemical instability. This study aimed to develop and optimize multi-layer self-nanoemulsifying pellets (ML-SNEP) to enhance the stability and dissolution of ramipril (RMP) and thymoquinone (THQ).
View Article and Find Full Text PDFInvestigation of aerosol jet printing for the preparation of solid dosage forms.
Int J Pharm
January 2025
EPSRC CMAC Future Manufacturing Research Hub, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 99 George Street, Glasgow G1 1RD UK; The Cancer Research UK Formulation Unit, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral St, Glasgow G4 0RE UK.
Oral drug delivery remains the preferred method of drug administration but due to poor solubility many active pharmaceutical ingredients (APIs) are ill suited to this. A number of methods to improve solubility of poorly soluble Biopharmaceutical Classification System (BCS) Class II drugs already exist but there is a lack of scalable, flexible methods. As such the current study applies the innovative technique of aerosol jet printing to increase the dissolution capabilities of a Class II drug in a manner which permits flexibility to allow dosage form tailoring.
View Article and Find Full Text PDFCharacteristics of Tylvalosin Tartrate Enteric Amorphous Pellets Prepared by Liquid Layering.
Pharm Res
January 2025
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Purpose: Tylvalosin Tartrate (TAT), a new-generation macrolide antibiotic, undergoes significant degradation in the stomach and in vivo rapid elimination upon oral administration, resulting in poor bioavailability. This study developed TAT enteric amorphous pellets by liquid layering (TAT/EAP-LL) with pH-sensitive and burst release characteristics, to enhance drug stability in the stomach and concentration enrichment in the duodenum.
Methods: The drug loading layer, isolation layer and enteric layer were formed on the surface of the blank core pellets.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!