Tenofovir alafenamide (TAF) is an antiretroviral (ARV) drug that is used for the management and prevention of human immunodeficiency virus (HIV). The clinical availability of ARV delivery systems that provide long-lasting protection against HIV transmission is lacking. There is a dire need to formulate nanocarrier systems that can help in revolutionizing the way to fight against HIV/AIDS. Here, we aimed to synthesize a polymer using chitosan and polyethylene glycol (PEG) by the PEGylation of chitosan at the hydroxyl group. After successful modification and confirmation by FTIR, XRD, and SEM, TAF-loaded PEGylated chitosan nanoparticles were prepared and analyzed for their particle size, zeta potential, morphology, crystallinity, chemical interactions, entrapment efficacy, drug loading, in vitro drug release, and release kinetic modeling. The fabricated nanoparticles were found to be in a nanosized range (219.6 nm), with ~90% entrapment efficacy, ~14% drug loading, and a spherical uniform distribution. The FTIR analysis confirmed the successful synthesis of PEGylated chitosan and nanoparticles. The in vitro analysis showed ~60% of the drug was released from the PEGylated polymeric reservoir system within 48 h at pH 7.4. The drug release kinetics were depicted by the Korsmeyer–Peppas release model with thermodynamically nonspontaneous drug release. Conclusively, PEGylated chitosan has the potential to deliver TAF from a nanocarrier system, and in the future, cytotoxicity and in vivo studies can be performed to further authenticate the synthesized polymer.

The objective is to develop immediate release buccal films of Eletriptan Hydrobromide (EHBR) using hydroxypropyl methylcellulose (HPMC) E5. The buccal films have the ability to disintegrate rapidly and provide both systemic and local effects. The solvent casting method was employed to prepare the films and the central composite rotatable design (CCRD) model was used for film optimization. All the formulated films were characterized for physicochemical evaluation (Fourier transform infrared spectroscopy (FTIR), X-ray Diffraction (XRD), differential scanning calorimetry (DSC), and Scanning electron microscopy (SEM), in in-vitro, ex-vivo, and in-vivo drug release. The fabricated films were transparent, colorless, and evenly distributed. The FTIR spectra showed no chemical interaction between the drug and excipients. In in-vitro analysis, the film has the highest% drug release (102.61 ± 1.13), while a maximum of 92.87 ± 0.87% drug was diffused across the cellulose membrane having a pore size of 0.45 µm. In the ex-vivo study, drug diffusion across the goat mucosa was performed and 80.9% of the drug was released in 30 min. In-vivo results depict a mean half-life (t½) of 4.54 ± 0.18 h and a C_max of 128 ± 0.87 (ng/mL); T_max was achieved in 1 h. Furthermore, instability and histopathological studies buccal films were proven to be safe and act as an effective dosage form. In a nutshell, optimized and safe instant release EHBR buccal films were prepared that have the tendency to provide effect effectively.

A migraine is a condition of severe headaches, causing a disturbance in the daily life of the patient. The current studies were designed to develop immediate-release polymeric buccal films of Eletriptan Hydrobromide (EHBR) and Itopride Hydrochloride (ITHC) to improve their bioavailability and, hence, improve compliance with the patients of migraines and its associated symptoms. The prepared films were evaluated for various in vitro parameters, including surface morphology, mechanical strength, disintegration test (DT), total dissolving time (TDT), drug release and drug permeation, etc., and in vivo pharmacokinetic parameters, such as area under curve (AUC), mean residence time (MRT), half-life (t_1/2), time to reach maximum concentration (T_max), and time to reach maximum concentration (C_max). The outcomes have indicated the successful preparation of the films, as SEM has confirmed the smooth surface and uniform distribution of drugs throughout the polymer matrix. The films were found to be mechanically stable as indicated by folding endurance studies. Furthermore, the optimized formulations showed a DT of 13 ± 1 s and TDT of 42.6 ± 0.75 s, indicating prompt disintegration as well as the dissolution of the films. Albino rabbits were used for in vivo pharmacokinetics, and the outcomes were evident of improved pharmacokinetics. The drug was found to rapidly permeate across the buccal mucosa, leading to increased bioavailability of the drug: C_max of 130 and 119 ng/mL of ITHC and EHBR, respectively, as compared to 96 (ITHC) and 90 ng/mL (EHBR) of oral solution. The conclusion can be drawn that possible reasons for the enhanced bioavailability could be the increased surface area in the form of buccal films, its rapid disintegration, and faster dissolution, which led toward the rapid absorption of the drug into the blood stream.

The buccal cavity may serve as a promising area to deliver the drug instantly. The route of drug administration helps to bypass the first-pass effect and hence to increase the drug bioavailability. Different types of dosage forms are available to deliver the drug through this route, and among them, instant release buccal films are of great interest when the rapid release of the drug and faster onset of action are required. This current study aimed to implement a statistical approach, Central Composite Rotatable Design (CCRD) to design and optimize immediate release buccal films of empagliflozin. HPMC E-5 and PVP K-30 were used as polymers, PEG 400 was used as a plasticizer, and Tween 80 was used as a surfactant. The drug was physically complexed with β-cyclodextrin to form a homogeneous mixture of the drug and other excipients. The films were prepared using an easy approach of the solvent casting method, followed by their physicochemical characterizations. The dissolution and permeation studies have been conducted using the USP-Dissolution apparatus II and Franz diffusion cell, respectively. The outcomes of the studies have suggested that the films were of uniform thickness and smooth texture and transparent in nature and exhibited good mechanical strength. The disintegration and dissolution tests assured rapid disintegration and dissolution of the films, leading to immediate release (approximately 90% within 10 min) of the drug, leading to rapid absorption and faster onset of action. The optimized formulation met all of the required parameters, ensuring reproducibility. Overall, the results concluded that the empagliflozin–β-cyclodextrin complex produced buccal films with good mechanical strength, uniform morphology, and immediate drug release via the buccal mucosa, fulfilling the study’s objectives.

High performance liquid chromatography (HPLC) is one of the commonly used techniques for the separation and quantification of various pharmaceuticals, both individually as well as in combination. The current studies were aimed to develop and validate a method for the simultaneous determination of methotrexate and leflunomide. These drugs are being used effectively for the treatment of rheumatoid and psoriatic arthritis. For simultaneous estimation of methotrexate and leflunomide, Shimadzu binary liquid gradient HPLC system, equipped with SPD-M40 photo diode array detector, DGU-20A _5R degassing unit, LC-20AD solvent delivery system, C18 column (4.6 mm × 250 mm, 5 µm) and, CTO-20AC oven, was used. Detection and quantification of both drugs were performed at 285 nm wavelength, using mobile phase, consisted of acetonitrile: water (65:35 v/v) along with 10% triethanolamine having adjusted pH 4.0 with ortho-phosphoric acid at a flow rate of 1.0 mL min ⁻¹ . The methotrexate and leflunomide were eluted at 1.99 and 6.45 min respectively, with sharp and distinguishing peaks. The Shimadzu's lab solution & Microsoft Excel 2016 was used for statistical analysis. The developed method was validated in accordance with USP and ICH guidelines Q2 (R1), for different parameters, including system suitability, specificity, linearity, range, accuracy, precision, LOD, LOQ, robustness and solution stability. The outcomes have confirmed that the method was validated with respect to studied parameters, as all of them were well within the specified limits.