Comparative Evaluation of Kollidon®VA64, SoluPlus®, and Aquasolve™ Hpmcas H-L Polymers: Impacts on Oral Spray Dried Powders Kollidon®VA64, SoluPlus® ve Aquasolve™ Hpmcas H-L Polimerlerinin Karşılaştırmalı Değerlendirmesi: Oral Püskürtülerek Kurutulmuş Tozlar Üzerindeki Etkileri

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OKTAY A. N., Polli J. E.

Fabad Journal of Pharmaceutical Sciences, cilt.50, sa.2, ss.355-370, 2025 (Scopus, TRDizin)

Özet

Ritonavir (RTV) is an anti-HIV protease inhibitor and antiretroviral medication to treat HIV /AIDS and especially COVID-19 infection. But it has low aqueous solubility which limits its oral bioavailability. Over the last decade, spray drying has become one of the most widely accepted solubility enhancement strategies in the pharmaceutical industry and academia. The spray drying process is a low-cost, solvent-based, scalable, continuous, and consistent technique to prepare an amorphous solid dispersion (ASD) of a hydrophobic drug in a single step. Even though the spray drying process has many advantages, it is a complicated system regarding process and formulation parameters. The formulation parameters such as the composition of feed (drug, polymeric carrier, and solvent) greatly impact the physicochemical properties of the spray-dried amorphous powder. Polymer selection is very crucial to developing a physiochemically stable and highly soluble ASD. However, there is a notable lack of comprehensive studies focusing on the impact of polymer type on spray dried powders. So, the objectives of this study were to perform a comparative evaluation of the impacts of Kollidon®VA64, SoluPlus®, and AquaSolve™ HPMCAS H-L polymers on spray-dried dispersion powders (SDP) of ritonavir. Powder characterization, DSC analysis, stability, solubility, and dissolution studies were performed. Short-term chemical stability studies supported that the RTV-ASD powders were stable for three months. The solubility of the coarse RTV crystalline powder was significantly increased through the ASD powders with various polymers, compared to the physical mixtures. Dissolution studies showed that the rank order was SoluPlus®>Kollidon®VA64>A quaSolve™ HPMCAS H-L SDPs for both inlet temperatures.