Comparative Evaluation of Kollidon®VA64, SoluPlus®, and Aquasolve™ Hpmcas H-L Polymers: Impacts on Oral Spray Dried Powders

Authors : Ayşe Nur Oktay, James Polli
Pages : 355-370
Doi:10.55262/fabadeczacilik.1662288
View : 41 | Download : 30
Publication Date : 2025-08-26
Article Type : Research Paper
Abstract :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 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 spray drying process has many advantages, it is complicated system regarding process and formulation parameters. The formulation parameters such as composition of feed (drug, polymeric carrier and solvent) greatly impacts the physicochemical properties of the spray dried amorphous powder. Polymer selection is very crucial to develop 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 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 by means of the ASD powders with various polymers, compared to the physical mixtures. Dissolution studies showed that rapid release profiles were obtained with SoluPlus®, Kollidon®VA64 and AquaSolve™ HPMCAS H-L.
Keywords : ritonavir, soluplus®, kollidon®va64, aquasolve™ hpmcas l:h, amorf katı dispersion

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