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Remdesivir is among the SARS-CoV-2 (severe acute respiratory syndrome coronavirus type 2) drugs with great potential. However, its poor aqueous solubility restricts its therapeutic action. Therefore, the aim was to develop the nasal delivery of Remdesivir with solubilizing polymers, poloxamer 407, and β-cyclodextrin, which resulted in significant solubility enhancement. In addition, this nanosuspension was developed for the first time for pulmonary delivery to enhance the in vivo performance of remdesivir. Remdesivir solubility and biocompatibility were greatly improved by polymeric encapsulation at the nanoscale. The nanosuspension was prepared by the modified precipitation-ultra sonication process and showed a good particle size 500 nm ± 20 nm, with polydispersity (0.226 ± 0.02) and zeta potential (-16.0 ± 2 mV). The nasal formulation was also assessed for in vitro dissolution and diffusion, in addition to toxicity investigations (Hemolysis, MTT assay). The conversion of remdesivir crystals to an amorphous form was verified by characterization studies (XRD and DSC). The morphology of the nano particles was determined by SEM method and found to be spherical and of uniform shape. FTIR study was performed to determine the drug compatibility with the polymers and was satisfactory. Histopathology study on goat nasal mucosa showed no adverse effects of the formulation on nasal tissues. Analysis using reverse transcription polymerase chain reaction revealed noticeably reduced levels of IL-4 mRNA expression (pro-inflammatory cytokines). In comparison to intravenous delivery, nasal delivery of remdesivir nanosuspension is patient-complaint and easy to use. The outcomes of this study demonstrate the potential for delivering remdesivir nanosuspension via the nasal route. [ABSTRACT FROM AUTHOR]

Polymeric blends are attractive drug delivery systems in the current era to provide controlled, pH-sensitive or targeted release of different drugs, and these blends can increase patient compliance by reducing dosing frequency. The aim of this research study was to prepare controlled release pH-sensitive okra gum/gelatin-based polymeric blend (OKMA-GEL) through aqueous polymerization method. The cytarabine (CYTB) was loaded in OKMA-GEL, to treat various cancerous diseases. Different ingredients (polymers (okra gum and gelatin), monomer (methacrylic acid—MAA), initiator (ammonium peroxodisulfate—APS) and cross-linker (methylene bisacrylamide—MBA)) were utilized to synthesize OKMA-GEL. Various techniques including FTIR, SEM, TGA, DSC and PXRD were applied on blend samples in concern of characterization. FTIR study depicted different functional groups and confirmed the successful development of polymeric blend. SEM indicated the presence of porous surface which is responsible for water imbibition into blend. TGA and DSC indicated enhanced thermal stability. PXRD of polymeric blend exhibited minor crystallinity and extensive amorphous nature. Swelling dynamics and drug release behaviors were observed at 1.2 pH and 7.4 pH. In this regard, better swelling and drug release were achieved at high pH (7.4) which endorsed a pH-responsive polymeric blend. Toxicity studies of drug unloaded polymeric blends were executed on rabbits which showed no toxic effect in findings. Conclusively, nontoxic OKMA-GEL was successfully synthesized that can be utilized for controlled release of CYTB. [ABSTRACT FROM AUTHOR]