Search

This research aimed to prepare and characterize a new type of polymeric cross-linked topical hydrogel patches for the treatment of wound infections. The free radical polymerization method was used to prepare the topical hydrogel patches by utilizing natural polymers, i.e., agarose and gelatin. These natural polymers were chemically cross-linked with monomer (acrylic acid) using ammonium persulfate as an initiator via the cross-linker N,N methylene bisacrylamide. An antibiotic, i.e., gentamicin sulfate was loaded into a designed polymeric system. The polymeric cross-linked topical hydrogel patches were made in a spherical shape, which was revealed to be stable and elastic. Fourier transform infrared spectroscopy, scanning electron microscopy, differential scanning calorimetry, thermogravimetric analysis, and X-ray powder diffraction investigation were used to characterize the topical hydrogel patches. Polymeric cross-linked hydrogel patches were evaluated for their sol–gel analysis, swelling studies, in vitro drug release studies against pH 5.5, 6.5, and 7.4, ex vivo drug permeation, and the deposition study on the rabbit’s skin by using a Franz diffusion cell. In addition, the skin irritation study and wound healing performance of drug-loaded topical patches were also assessed and compared to commercially available formulations. The topical hydrogel patches were found to be non-irritating to the skin for up to 72 h as determined by a Draize patch test and when compared to marketed formulations, these topical patches resulted in faster wound healing. The prepared formulation showed promising potential for the treatment of skin wound infection.

Objective of the research was to potentiate solubility of Rosuvastatin by nanogels synthesized by free radical polymerization. Surface morphology and structural compatibility were studied through scanning electron microscopy (SEM) and Fourier Transform Infrared (FTIR) spectroscopy. Zeta sizer was used for particle size analysis. Swelling, in-vitro release and solubility studies were accomplished in different media. Similarly, results of in-vitro release of nanogels and commercially available tablets of Rosuvastatin were compared in different dissolution media. Biocompatibility study was performed in healthy rabbits for safety profile. FTIR spectroscopy confirmed the presence of corresponding peaks of respective functional groups of individual constituents and that of the drug in unloaded and loaded nanogels. SEM images depicted the fluffy appearance of nanogels with small pores inside the structure. Particle size of the optimized formulation was in the range of 217.70 ± 2.23 for unloaded and 257.33 ± 2.11 for loaded nanogels. Percent drug loading, in-vitro drug release and solubility profiles were also satisfactory. In comparison with commercially available tablet Rovista®, in-vitro release profiles of synthesized nanogels showed better response. Moreover, synthesized nanogels were also biocompatible. It was concluded that the solubility of Rosuvastatin was potentially enhanced by nanogels and such formulation can also be used for other poorly soluble drugs. [ABSTRACT FROM AUTHOR]

A hydrogel topical patch of neomycin was developed by using sodium alginate (SA) and hydroxyethylcellulose (HEC) as polymers. Free radical polymerization in an aqueous medium was initiated by using acrylic acid (AA) and N,N′-methylenebisacrylamide (MBA). Prepared hydrogels were characterized for pH sensitivity and sol–gel analysis. In addition, the effect of reactant contents on the developed formulation was evaluated by swelling behavior. SEM assay showed the rough structure of the hydrogel-based polymeric matrix, which directly enhances the ability to uptake fluid. FTIR spectra revealed the formation of a new polymeric network between reactant contents. TGA and DSC verified that fabricated polymeric patches were more thermodynamically stable than pure components. Gel fractions increased with increases in polymer, monomer, and cross-linker contents. The swelling study showed the pH-dependent swelling behavior of patches at pH 5.5, 6.5, and 7.4. The release pattern of the drug followed zero-order kinetics, with diffusion-controlled drug release patterns according to the Korsmeyer–Peppas (KP) model. Ex vivo studies across excised rabbit skin verified the drug retention in the skin layers. The hydrogel patch effectively healed the wounds produced on the rabbit skin, whereas the formulation showed no sign of irritation on intact skin. Therefore, neomycin hydrogel patches can be a potential candidate for controlled delivery for efficient wound healing. [ABSTRACT FROM AUTHOR]

The main objective of the current research work was to fabricate polyethylene glycol-based hydrogels for the controlled delivery of Ketorolac. Polyethylene glycol was chemically cross-linked with acrylic acid using 2-hydroxyethyl methacrylate as a cross-linker with ammonium persulfate and sodium metabisulphite as initiators. To determine the efficiency of the synthesized system, it was subjected to various structural characterization, such as Fourier transform infrared spectroscopy, Differential scanning calorimetry, Thermogravimetric analysis, and Scanning electron microscopy. All the results obtained from structural characterizations confirmed a well-cross-linked, thermally stable, and a porous system. Swelling and in-vitro release studies performed in pH 1.2 and 7.4 showed pH responsiveness as more swelling and drug release were observed in pH 7.4 as compared to pH 1.2. The drug release was considered as non-Fickian transport from kinetic modeling and partially controlled by the viscoelastic relaxation of hydrogel. Sol-gel fraction depicted that gel content was increased as the concentrations of the polymer, monomer, and cross linker were increased. Similarly, the results obtained from stability studies confirmed a stable synthesized system. Moreover, statistical analysis was also employed for a better comparison of the swelling and in-vitro results. [ABSTRACT FROM AUTHOR]

The present study was conducted to fabricate and characterize mucilage-based polymeric networks of Aloe vera for controlled drug release. Aloe vera mucilage was used to develop a polymeric network via the free-radical polymerization method using potassium persulphate as the initiator, N′ N′-Methylene bisacrylamide as the crosslinker, and acrylamide as the monomer. Using varying concentrations of Aloe vera mucilage, crosslinker, and monomer, we developed different formulations. Swelling studies were conducted at pH 1.2 and 7.4. Concentrations of polymer, monomer, and crosslinker were optimized as a function of swelling. Porosity and gel content were calculated for all samples. FTIR, SEM, XRD, TGA, and DSC studies were conducted for the characterization of polymeric networks. Thiocolchicoside was used as a model drug to study the in vitro release in acidic and alkaline pH. Various kinetics models were applied by using a DD solver. Increasing content of monomer and crosslinker swelling, porosity, and drug release decreased while gel content increased. An increase in Aloe vera mucilage concentration promotes swelling, porosity, and drug release of the polymeric network but decreases gel content. The FTIR study confirmed the formation of crosslinked networks. SEM indicated that the polymeric network had a porous structure. DSC and XRD studies indicated the entrapment of drugs inside the polymeric networks in amorphous form. The analytical method was validated according to ICH guidelines in terms of linearity, range, LOD, LOQ, accuracy, precision, and robustness. Analysis of drug release mechanism revealed Fickian behavior of all formulations. All these results indicated that the M1 formulation was considered to be the best polymeric network formulation in terms of sustaining drug release patterns. [ABSTRACT FROM AUTHOR]

Present study was carried out to analyze the impact of three different monomers on release of losartan potassium from graft polymeric network prepared through free radical polymerization. N, N-methylene bis acrylamide was used as crosslinker and potassium persulfate as initiator. Losartan potassium as used as model drug because, it has very small plasma half-life and wide range of applications as an effective and efficient ARB (Angiotensin II Receptor Blockers) causing lower incidence of side - effects. Influence of three different monomers on swelling and in vitro drug release of the delivery system was evaluated at pH 1.2 and 7.4. The polymeric networks were characterized by Fourier transform infrared spectroscopy, Thermogravimetric analysis and Scanning electron microscopy. Polymeric network prepared with acrylic acid and methacrylic acid showed pH responsive behavior and while acrylamide based nexus exhibited pH independent style in swelling and drug release. However, among all the formulations, maximum swelling ratio (25.86) and optimal prolonged drug release (82.92%) was observed for GG-co-AA (M2) polymeric network at intestinal pH 7.4. The results indicated that GG-co-AA polymeric network could be an impending pH-sensitive drug delivery system for Losartan potassium. (M2) designated as formulation code with varying acrylic acid contents [ABSTRACT FROM AUTHOR]

The present study was conducted to fabricate and compare pH-sensitive polymeric networks of Artemisia vulgaris- Methacrylic acid using free radical polymerization conventional method and microwave-assisted method. Potassium persulphate and N’ N’- Methylene bisacrylamide were employed as an initiator-crosslinker system. Swelling studies were performed at pH 1.2, 4.5, 6.8 and 7.4. Concentrations of polymer and monomer along with radiation dose were optimized as a function of swelling. Porosity and gel fraction were calculated for all samples. FTIR study confirmed the formation of cross-linked networks. Results of SEM indicated that the microwave irradiated polymeric network had a more porous structure. DSC and XRD study indicated the entrapment of drug inside the polymeric networks in amorphous form. In comparison to the conventional method, the polymeric network prepared by the microwave-assisted method exhibited high swelling ratios, porosity, thermal stability and drug release. These results signify microwave radiations as an effective alternative to the conventional heating method. [ABSTRACT FROM AUTHOR]

Natural mucilages are auspicious biodegradable polymeric materials. The aim of the present research work was to elucidate the characteristics of quince mucilage-based polymeric network for sustained delivery of metprolol tartrate and its toxicity evaluation. Mucilage was extracted by hot water extraction, and characterization of quince mucilage was accomplished by using Fourier transform infrared (FTIR) spectroscopy. Different batches of quince mucilage polymeric network were prepared by free radical polymerization by utilizing varying ratios of quince mucilage, acrylamide and crosslinker. Degree of swelling depends on concentration of mucilage, monomer and also on crosslinking density of polymeric network. FTIR illustrates proficient grafting, and morphological (scanning electron microscopy) analysis signified porous design. Hence, quince mucilage-based design was encouraging for sustained delivery of metprolol tartrate and acute toxicity evaluation proved that mucilage-based network was safe for oral drug delivery system. [ABSTRACT FROM AUTHOR]

Routinely used anti-inflammatory drugs are associated with off-target effects such as cyclooxygenase (COX)- 1 inhibition and gastric ulcers. The aim of this study is to examine the anti-inflammatory potential and gastroprotective effects of synthetic amino acid derivatives of 2-mercaptobenzimidazole (MBAA1, MBAA2, MBAA3, MBAA4 and MBAA5). The results showed that compound MBAA5 possess a potential anti-inflammatory action by inhibition of 15- LOX and COX-2. MBAA5 also attenuated the pro-inflammatory cytokines and mediators (TNF-α, IL-1β and COX-2) in rat hind paw in carrageenan-induced inflammatory model of rat. 2-mercaptobenzimidazole derivative, MBAA5 also inhibited gastric H+/K+ ATPase and demonstrated a better selectivity index for COX-2 (SI 27.17) in comparison to celecoxib (SI 41.43). Molecular docking studies predicted the binding interactions of the synthesized compounds with retrieved target proteins of H+/K+ ATPase, COX-1, COX-2, and 15-LOX. The results of in silico and molecular docking analysis of amino acid derivatives of 2-mercaptobenzimidazoles further explained their pharmacological activities. Moreover, these compounds presented better antimicrobial activity against three clinical isolates of Helicobacter pylori. Together, our findings suggested that these synthetic 2-mercaptobenzimidazole derivatives are safer therapeutic candidates for inflammation. [ABSTRACT FROM AUTHOR]

Benzimidazole is an important pharmacophore for clinically active drugs against inflammation and treatment of pain, however, it is associated with gastrointestinal side effects. Here we synthesized benzimidazole based agents with significant analgesic/anti‐inflammatory potential but with less gastrointestinal adverse effects. In this study, we synthesized novel, orally bioavailable 2‐mercaptobenzimidazole amino acid conjugates (4a–4o) and screened them for analgesic, anti‐inflammatory and gastro‐protective effects. The synthesized 2‐mercaptbenzimidazole derivatives were characterized for their structure using FTIR, 1H NMR and 13C NMR spectroscopic techniques. The 2‐mercaptobenzimidazole amino acid conjugates have found to possess potent analgesic, anti‐inflammatory and gastroprotective activities, particularly with compound 4j and 4k. Most of the compounds exhibited remarkable anti‐ulcer and antisecretory effects. Molecular docking studies were carried out to study the binding affinities and interactions of the synthesized compounds with target proteins COX‐2 (PDB ID: 3LN1) and H+/K+‐ATPase (PDB ID: 5Y0B). Our results support the clinical promise of these newly synthesized 2‐mercaptobezimidazol conjugates as a component of therapeutic strategies for inflammation and analgesia, for which the gastric side effects are always a major limitation. [ABSTRACT FROM AUTHOR]

In the present study, we synthesized silver (Ag) nanoparticles using aqueous extracts of clove (Syzygium aromaticum) (SAE). This synthesis of green silver nanoparticles (AgNP) was a novel and effectual tool against the Newcastle Viral Disease (NDV). Syzygium aromaticum extract was used as reducing and stabilizing agent for synthesis of silver nanoparticles. AgNP were characterized using diversity of biophysical methods inclusive of Fourier transform infrared spectroscopy (FTIR), UV-VIS spectroscopy and Transmission electron microscopy (TEM) for morphology and size. Furthermore, XRD analysis confirmed the crystalline nature of the particles. In current investigations, the antiviral activity of clove buds silver nanoparticles was inspected in-vitro and in-ovo. Embryonated chicken eggs were used to perform the cytotoxicity assay of the clove extract silver nanoparticles (CESN). CESN showed in vitro antiviral activity against NDV in embryonated eggs. [ABSTRACT FROM AUTHOR]

Xanthan gum-based hydrogel formulation FXG3 was prepared by a free radical polymerization technique. To assess the safety of FXG3 hydrogel for potential application as a new drug delivery system, a single oral dose toxicity study was conducted according to OECD guidelines. Female adult rats of Wistar strain were divided into group A and group B. Group A served as the control and was given 1 mL/100 g body weight 0.9% saline. Group B received a dose of 5 g/kg body weight of FXG3 hydrogel. Rats were observed continuously for 14 days for clinical signs, and prior to terminal sacrifice, blood samples were taken to assess for hematology and biochemical parameters. Selected organs (heart, liver, lung, kidneys, spleen, and stomach) were removed and examined macroscopically, washed, sliced and stained with hematoxylin-eosin for histopathological investigation. No mortality or any signs of acute toxicity was observed during the observation period. No macroscopic alteration was found in the selected organs. Histopathological examination did not show any pathological changes. Thus, the maximal tolerated dose of FXG3 was calculated to be higher than 5 g/kg body weight. It can be concluded that FXG3, a xanthan gum-based hydrogel formulation, was non-toxic after acute oral administration at 5 g/kg body weight, and thus may be a promising candidate in controlled drug delivery system. [ABSTRACT FROM AUTHOR]

The main objective of the present study was to explore the potential of matrix tablets as extended release dosage form of tianeptine, using HMPC K100 as a polymer. HPMC K100 extended the release of the drug from formulation due to the gel-like structure. Direct compression method was adopted to compress the tablets using different concentrations of polymer. Tablets were evaluated for pre-compression and post-compression parameters. Drug release study showed that tablet extends the release of drug with the increasing concentration of polymer. Drug, polymers and tablets were analyzed and/or characterized for compatibility, degradation, thermal stability, amorphous or crystalline nature via FTIR, DSC, TGA, XRD studies. SEM study predicted that tablets had a uniform structure. HPMC K100 based tablets were similar to that of the reference product. Acute toxicity study conducted on Swiss albino mice showed that matrix tablets were safe and non-toxic, as no changes in physical activity and functions of organs were observed. Biochemical and histopathological study revealed lack of any kind of abnormality in liver and renal function. Moreover, necrotic changes were absent at organ level. [ABSTRACT FROM AUTHOR]

A rapid, sensitive and simple reversed-phase high-performance liquid chromatographic (HPLC) method has been developed and validated for the determination of acyclovir (ACV) in rabbit plasma. BDS C18 column was used to conduct analysis using ammonium dihydrogen phosphate buffer (50 mM) and methanol as mobile phase (98 : 2), with pH adjusted to 2.5 using orthophosphoric acid. The flow rate was kept at 1 mL/min. Selective precipitation of plasma proteins was done by adding 5% perchloric acid. Precipitated plasma proteins were separated by centrifugation. ACV moves in a supernatant, which was snapped and passed through a syringe filtration assembly. Direct injection of supernatant was given into a BDS C18 column and ACV was detected at 256 nm. The limit of detection for ACV in plasma was estimated as 15 ng/mL whereas the limit of quantitation was calculated as 25 ng/mL. Moreover, the developed method has been found to be selective and linear into concentration range of 25-2000 ng/mL. The present method could be successfully applied to samples from bioavailability and bioequivalence studies. [ABSTRACT FROM AUTHOR]