In the present study pH-sensitive polyvinylpyrrolidone/acrylic acid (PVP/AA) hydrogels were synthesized by free radical polymerization in the presence of ethylene glycol dimethacrylate (EGDMA) as a...

We report synthesis, characterization, and drug release attributes of a series of novel pH‐sensitive poly(acrylic‐co‐vinylsulfonic) acid hydrogels. These hydrogels were prepared by employing free radical polymerization using ethylene glycol dimethacrylate (EGDMA) and benzyl peroxide (BPO) as cross‐linker and initiator, respectively. Effect of acrylic acid (AA), polyvinylsulfonic acid (PVSA), and EGDMA on prepared hydrogels was investigated. All formulations showed higher swelling at high pHs and vice versa. Formulations containing higher content of AA and EGDMA show reduced swelling, but one with higher content of PVSA showed increased swelling. Hydrogel network was characterized by determining structural parameters and loaded with isosorbide mononitrate. FTIR confirmed absence of drug polymer interaction while DSC and TGA demonstrated molecular dispersion of drug in a thermally stable polymeric network. All the hydrogel formulations exhibited a pH dependent release of isosorbide mononitrate which was found to be directly proportional to pH of the medium and PVSA content and inversely proportional to the AA contents. Drug release data were fitted to various kinetics models. Results indicated that release of isosorbide mononitrate from poly(AA‐co‐VSA) hydrogels was non‐Fickian and that the mechanism was diffusion‐controlled.

Artemisinin (ART) is a sesquiterpene lactone with an endo-peroxide bridge that is thought to be responsible for its antimalarial activity. It has low oral bioavailability because of aqueous insolubility, which leads to local toxicity at the site of aggregation. The present work focused on increasing its solubility and evaluating its permeation across a model membrane to mimic transdermal delivery that bypasses the hepatic metabolism. For this purpose, physical mixtures (PM), solid dispersions (SD) and lyophilized dispersions (LD) with different drug-polymer ratios (1:0.5, 1:1, 1:2, 1:4 and 1:9) were prepared using the hydrophilic polymer polyvinylpyrrolidone (PVP). Drug-polymer dispersions were characterized using X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). Solubility was measured in three solvents: de-ionized water, phosphate buffered saline (PBS) and methanol. The toluene-water partition coefficient was evaluated and compared with the literature and calculated logP values. In vitro diffusion of ART was studied across a polydimethylsiloxane membrane from a saturated solution of drug-polymer dispersions. XRD patterns showed a gradual decrease in crystallinity of ART with increasing polymer concentration, while FTIR confirmed no interactions between ART and PVP. Solubility was increased up to 4-, 5- and 8-fold for LD in water, PBS and methanol, respectively. The logP for toluene-water was 2.65 ± 0.3, which is in good agreement with literature and calculated logP values. Permeation was enhanced, which is attributed to the decrease in crystallinity and increase in wettability of the drug. The ART flux was significantly higher than that of pure ART (0.12 ± 0.01) with increasing PVP concentration for SD and LD formulations. In conclusion, drug-polymer dispersions with PVP improve the pharmaceutical properties of ART in the order LD>SD>PM.

Background: Bezafibrate is a BCS class II drug as it presents very low solubility in water; therefore, its bioavailability after oral administration is very poor. The aim of this work was to enhance solubility and dissolution rate of bezafibrate in water in order to enhance its oral bioavailability. Methods: Several formulations were prepared using PVP K30 and Cremophor ELP employing the solvent-evaporation method and the electrospraying technique. Solubility, release rate, bioavailability in male Sprague Dawley rats, and lipid profile attributes in Wistar rats were assessed in comparison with bezafibrate plain powder. Solid-state characterization was carried out using X-ray diffraction (XRD) analysis, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM). Results: All the formulations exerted positive effect towards the desired goal. In particular, the optimized formulation furnished about 14-fold enhanced solubility and 85.48 ± 10.16% drug was released in 10 min as compared with bezafibrate alone (4.06 ± 2.59%). The drug existed in the amorphous state in the prepared sample as confirmed by XRD and DSC, whilst no drug-excipient interactions were observed through FTIR analysis. Moreover, SEM revealed smooth-surfaced spherical particles of the optimized formulation. A 5.5-fold higher oral bioavailability was achieved with the optimized formulation in comparison with bezafibrate plain powder. Also, TG, LDL and TC were decreased, and HDL was increased considerably in HFD-treated rats. Conclusion: The optimized formulation consisting of bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w) might be a capable drug delivery system for orally administering poorly water-soluble bezafibrate with improved bioavailability and antihyperlipidemic effects.

Mounting‐up economic losses to annual crops yield due to micronutrient deficiency, fertiliser inefficiency and increasing microbial invasions (e.g. Xanthomonas cempestri attack on tomatoes) are needed to be solved via nano‐biotechnology. So keeping this in view, the authors’ current study presents the new horizon in the field of nano‐fertiliser with highly nutritive and preservative effect of green fabricated zinc oxide‐nanostructures (ZnO‐NSs) during Lycopersicum esculentum (tomato) growth dynamics. ZnO‐NS prepared via green chemistry possesses highly homogenous crystalline structures well‐characterised through ultraviolet and visible spectroscopy, Fourier transform infrared spectroscopy, X‐ray diffraction and scanning electron microscope. The ZnO‐NS average size was found as small as 18 nm having a crystallite size of 5 nm. L. esculentum were grown in different concentrations of ZnO‐NS to examine the different morphological parameters includes time of seed germination, germination percentage, the number of plant leaves, the height of the plant, average number of branches, days count for flowering and fruiting time period along with fruit quantity. Promising results clearly predict that bio‐fabricated ZnO‐NS at optimum concentration resulted as growth booster and dramatically triggered the plant yield.