In this study, we fabricated pH-sensitive polyvinylpyrrolidone/acrylic acid (PVP/AA) hydrogels by a free-radical polymerisation method with variation in the content of monomer, polymer and cross-linking agent. Swelling was performed in USP phosphate buffer solutions of pH 1.2, 5.5, 6.5 and 7.5 with constant ionic strength. Network structure was evaluated by different parameters and FTIR confirmed the formation of cross-linked hydrogels. X-ray crystallography showed molecular dispersion of tramadol HCl. A drug release study was carried out in phosphate buffer solutions of pH 1.2, 5.5 and 7.5 for selected samples. It was observed that swelling and drug release from hydrogels can be modified by changing composition and degree of cross-linking of the hydrogels under investigation. Swelling coefficient was high at higher pH values except for the one containing high PVP content. Drug release increased by increasing the pH of the medium and AA contents in hydrogels while increasing the concentration of cross-linking agent had the opposite effect. Analysis of the drug release mechanism revealed non-Fickian transport of tramadol from the hydrogels.Uniterms: Drugs/release. Hydrogels/pH sensitive. Polyvinylpyrrolidone-acrilic acid/hidrogels. Tramadol hydrochloride. Methylene bisacrylamide.Nesse estudo, preparamos hidrogéis de polivinilpirrolidona/ácido acrílico(PVP/AA), sensíveis ao pH, por meio de método de polimerização de radical livre, com variações no conteúdo de monômero, de polímero e de agente de ligação cruzada. O inchamento foi realizado em soluções tampão fosfato USP pH 1,2, 5,5, 6,5 e 7,5, com força iônica constante. A estrutura reticular foi avaliada por diferentes parâmetros e o FTIR confirmou a formação de hidrogéis de ligação cruzada. A cristalografia de raios X mostrou dispersão molecular do cloridrato de tramadol. Realizou-se estudo de liberação do fármaco em soluções tampão fosfato pH 1,2, 5,5 e 7,5 para amostras selecionadas. Observou-se que o inchamento e a liberação do fármaco dos hidrogéis podem ser modificados mudando-se a composição e o grau de ligação cruzada dos hidrogéis em estudo. O coeficiente de inchamento foi alto em pH mais altos, exceto para um deles com alto conteúdo de PVP. A liberação do fármaco aumentou com o aumento do pH do meio e do conteúdo em AA nos hidrogéis, enquanto que o aumento na concentração do agente de ligação cruzada apresentou efeito oposto. A análise do mecanismo de liberação do fármaco revelou transporte não Fickiano do tramadol dos hidrogéis.

Background: Fruit peels are considered as waste and contribute towards a major proportion of biomass. They might be a good source of various therapeutic benefits. Peels biomass of citrus fruits are usually considered as garbage. Such peels may have many important and valuable medicinal components with pharmacological activities. Citrus reticulata, (of family Rutaceae, local name tangerine) is a local seasonal fruit in Pakistan which is a very good example regarding wastage of its peels. Objective: The study is based on exploration of a citrus fruit peel derived essential oil, its chemical characterization, identification of various bioactive components and the exploration of pharmacological potentials (antibacterial and wound healing activity). Method: Essential oil was recovered by hydro-distillation of freshly collected peels. Chemical constituents of oil were determined by gas chromatography-mass spectroscopy (GC-MS) analysis. Antioxidant activities were evaluated by total phenolic contents, total flavonoid content, DPPH scavenging activity and reducing power assay. Antibacterial activity was determined using disc diffusion assay. In vivo wound healing potential was determined in rabbits after topical administration of oil. Wound scoring was calculated followed by histological study. Results: GC-MS analysis showed presence of various components with greatest proportion of D-Limonene (89.31%). Total flavonoid and phenolic contents were found to be 14.63 ± 0.95 mg CE/g and 17.03 ± 3.24 mg GAE/g respectively while DPPH activity was found to be 73.32%. Better antibacterial activity was shown against E. coli. In vivo studies showed significant reduction in wound diameter in essential oil treatment groups. Further the essential oil was found non-irritant in draize scoring. Conclusion: The study concluded that essential oil of this fruit peel might be used for antibacterial and wound healing purposes.

Background: Peganum harmala is traditionally used to manage rheumatoid arthritis (RA) and other inflammatory conditions. However, its use against RA has not been scientifically evaluated. The current study was designed to assess the anti-arthritic and anti-inflammatory activities of the methanolic extract of P. harmala leaves by in vitro and in vivo methods. Methods: The in vitro assays were carried out to determine the effect of plant extract on inhibition of egg albumin denaturation and human red blood cell membrane (HRBC) stabilization. Moreover, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity was performed to determine the antioxidant potential. In vivo anti-arthritic activity was performed by determining the curative effect against Complete Freund’s adjuvant (0.1 ml). The plant extract was administered to rats orally at 200, 400 and 600 mg/kg/day for 21 days. Results: The values of IC50 of plant extract in protein denaturation, stabilization of HRBC and DPPH assays were 77.54 mg/ml, 23.90 mg/ml and 58.09 µg/ml respectively. Moreover, the plant extract significantly attenuated the poly-arthritis and weight loss, anemia and paw edema. The plant extract restored the level of C-reactive protein, rheumatoid factor, alanine transaminase, aspartate transaminase and alkaline phosphatase in poly-arthritic rats. Moreover, the plant extract restored the immune organs weight in treated rats. Treatment with P. harmala also significantly subdued the oxidative stress by reinstating superoxide dismutase, reduced glutathione, catalase and malondialdehyde in poly-arthritic rats. The plant extract notably restored the prostaglandin-E2 and tumor necrosis factor (TNF)-α in the serum of poly-arthritic rats. Conclusion: It was concluded that P. harmala extract had potential antioxidant, anti-inflammatory and antiarthritic activities which primarily might be attributed to alkaloids, flavonoids and phenols.

Background: Tylophora hirsuta Wall. has long been used as traditional medicine for the treatment of diabetes. Current study is designed to evaluate the antidiabetic and anti-inflammatory activity of different extracts of aerial parts of Tylophora hirsuta. Methods: Sequential maceration was conducted to obtain extracts. Total phenolic contents were determined by FolinCiocalteau method. The antioxidant activity was assessed by DPPH free radical scavenging assay. The extracts were tested for its inhibitory activity against α-amylase in-vitro. In-vivo anti diabetic assay was conducted using alloxan induced diabetic model and OGTT was conducted on normal rats. ELISA was used to determine the proinflammatory cytokines (TNF-α and IL-6). Polyphenolic composition of the extract was analyzed using a HPLC system. Results: Aqueous extract exhibited highest total phenolic contents (985.24± 3.82 mg GAE/100 g DW), antioxidant activity (IC50 = 786.70 ± 5.23 Conclusion: These results showed that Tylophora hirsuta possess strong antidiabetic and anti-inflammatory potentials and justify its folklore use for the management of diabetes.

Fenbfen is used for pain, pyrexia and in the management of osteoarthritis, rheumatoid arthritis and other musculoskeletal disorders. The present research was planned to examine the immunomodulatory activity of fenbufen in different models of cell-mediated immunity (CMI) and humoral immunity (HI). The CMI was evaluated by delayed-type hypersensitivity (DTH) and cyclophosphamide-induced neutropenia assays while HI was appraised by hemagglutination (HA) assay by administering fenbufen at 2, 6 and 10 mg.kg-1 and azathioprine 40 mg.kg-1 (as standard therapy) to albino mice by intraperitoneal route. The ex vivo immunomodulatory action was determined by red blood cell (RBC) membrane stabilization and protein denaturation assays. The results showed that fenbufen treatment had significantly (p<0.05-p<0.001) reduced white blood cells, hemoglobin content, and red blood cells in the healthy and neutropenic mice. A significant (p<0.001) reduction in activities of superoxide dismutase and catalase and glutathione contents, and enhancement of malondialdehyde level were observed in neutropenic mice that were restored by fenbufen treatment. It suppressed DTH reaction after 24, 48 and 72 h post topical application of 2, 4-dinitrofluorobenzene (DNFB). Fenbufen or azathioprine treated groups also showed a significant reduction in the antibody titer against human RBCs induced immune activation in mice as compared to the disease control mice. Fenbufen showed IC50 of 14.0, 50.5 and 66.2 μg.ml-1 whereas, diclofenac sodium showed IC50 of 61.0, 126 and 50.5 μg/ml in RBCs membrane stabilization, egg albumin and bovine serum albumin denaturation assays respectively. The current study shows that fenbufen might have potential immunomodulatory activity against CMI and HI. It can be utilized to treat immune system disorders.