Cationic Chitosan/Pectin Polyelectrolyte Nanocapsules of Moxifloxacin as Novel Topical Management System for Bacterial Keratitis.

PURPOSE: Moxifloxacin (MOX) is a fourth-generation fluoroquinolone and a broad spectrum antibiotic used in the management of bacterial keratitis (BK). This investigation aimed to formulate MOX-loaded chitosan/pectin cationic polyelectrolyte nanocapsules (CPNCs) for the effective topical treatment of BK. METHODS: Physicochemical properties like nanocapsule size, charge, drug entrapment efficiency (EE), viscosity, pH, and in-vitro release profile of CPNCs were evaluated. The in-vitro antibacterial activity of CPNCs and marketed formulations (MFs) was studied against Staphylococcus aureus. Ex-vivo corneal permeation studies of CPNCs were evaluated with the help of a modified diffusion apparatus, which was used with goat cornea. The pharmacodynamic study was performed with optimized CPNCs on a BK-induced rabbit eye model and compared with MF. RESULTS: The optimized nanocapsules appeared as positive charge (+19.91 ± 0.66) with a nano size (242.0 ± 0.30 nm) as calculated by the dynamic light scattering method. The in-vitro release profile of CPNCs exhibited sustained release properties. The ex-vivo permeation pattern also supported the improved drug permeation through the cornea from CPNCs as compared with MF. Draize irritation studies confirmed that the prepared formulation is compatible with the corneal tissue. The in-vivo study concluded that the antibacterial activity of CPNCs was improved when evaluated with MF. CONCLUSION: The obtained results showed that CPNCs were the better choice for the management of BK therapy due to its capability to improve the corneal adhesion of CPNCs through direct interaction with the mucous membrane of the corneal tissue.

Immunomodulatory Study of Different Solvent Extract of Elephantopus scaber Linn.

The aim and objective of present study is that to provide a scientific evidence for the immunomodulatory potential of Elephantopus scaber in vivo. The immunomodulatory activity was performed in petroleum ether, solvent ether, methanol and aqueous extract of aerial part and root of E. scaber by using models such as delayed type hypersensitivity, humoral antibody response to SRBC and carbon clearance test for phagocytic activity in Wistar rat. The observation and results of present study suggested that among the total 8 extract, only the petroleum ether and solvent ether aerial part extract of E. scaber significantly decreased in delayed type hypersensitivity (DTH), humoral antibody (HA) titre and phagocytic index thereby indicating significant immunosuppressant activity in experimental animals.

Protective effects of piperine against copper-ascorbate induced toxic injury to goat cardiac mitochondria in vitro.

Piperine, the main alkaloid of black pepper, Piper nigrum Linn., is an important Indian spice used in traditional food and medicine in India. In the present study, we investigated the antioxidant activities of piperine against copper-ascorbate induced toxic injury to mitochondria obtained from a goat heart, in vitro. Incubation of isolated cardiac mitochondria with copper-ascorbate resulted in elevated levels of lipid peroxidation and protein carbonylation of the mitochondrial membrane, a reduced level of mitochondrial GSH and altered status of antioxidant enzymes as well as decreased activities of pyruvate dehydrogenase and the Kreb's cycle enzymes, altered mitochondrial morphology, mitochondrial swelling, di-tyrosine level and mitochondrial DNA damage. All these changes were found to be ameliorated when the cardiac mitochondria were co-incubated with copper-ascorbate and piperine, in vitro. Piperine, in our in vitro experiments, was found to scavenge hydrogen peroxide, superoxide anion free radicals, hydroxyl radicals and DPPH radicals, in a chemically defined system, indicating that this compound may provide protection to cardiac mitochondria against copper-ascorbate induced toxic injury through its antioxidant activities. The results of this study suggest that piperine may be considered as a future therapeutic antioxidant and may be used singly or as a co-therapeutic in the treatment of diseases associated with mitochondrial oxidative stress.

A review on pharmacology and toxicology of Elephantopus scaber Linn.

Elephantopus scaber Linn., family Asteraceae, is a small herb found in the Neotropics, Europe, Asia, Africa and Australia. The parts of this plant have been used traditionally for the treatment of number of diseases in many countries. The plant has been extensively screened for anticancer activity. Sesquiterpene lactones such as deoxyelephantopin, isodeoxyelephantopin, scabertopin and isoscabertopin. have been found to be prominent anticancer constituents. Many other biological activities such as antimicrobial, hepatoprotective, antioxidant, antidiabetic, anti-inflammatory, analgesic, antiasthamatic, antiplatelet and wound healing ability have been reported in various research articles. This review has been envisaged with an intention to provide the scientific information about the pharmacological and toxicological profile of E. scaber.

Evaluation of immunomodulatory potential of ethanolic extract of Roscoea procera rhizomes in mice.

PURPOSE: The aim of present study was to evaluate immunomodulatory potential of ethanolic extract of Roscoea procera (Zingiberaceae) rhizomes by using delayed-type hypersensitivity (DTH) and carbon clearance method in comparison to standard established immunosuppressant drug, cyclophosphamide (30 mg/kg, i.p.) in mice. MATERIAL AND METHODS: The extract was comprised to acute toxicity (OECD-423 guideline), DTH and carbon clearance method for their immunomodulatory potential. Ethanolic extract of Roscoea procera rhizomes administered orally at doses 300 mg/kg and 600 mg/kg, p.o. to mice. RESULT AND CONCLUSION: Result of our study revealed that, the foot pat thickness of ethanolic extract group (P<0.05) significantly enhanced the production of circulating antibody titre in response to Sheep red blood cells (SRBC) and phagocytic functions of mononuclear macrophages and non-specific immunity. Result were also supported by serological and haematological tests data. Hence, the present investigation reveals that, ethanolic extract of Roscoea procera rhizomes possesses immunostimulant properties. Further studies to identify the active moieties and elucidation of the mechanism of action are recommended.

Development and evaluation of formulations of microbial biotransformed extract of tobacco leaves for hair growth potential.

BACKGROUND: Extensive researches are going on to explore the effective and safe drug for their hair growth. Tobacco leaves are traditionally known to potentiate hair growth promotion. Therefore, the aim of present study was to formulate and evaluate the microbial biotransformed extract of tobacco leaves for hair growth potential in male albino wister rats. MATERIALS AND METHODS: The extract of was prepared by microbial biotransformation of tobacco leaves in cow urine for 28 days. The herbal formulations (lotion) were formulated by general method using o/w type base in various rations or concentrations such as 10%, 20% and 30% of extract. These lotions were applied on shaved skin area of rats for 30 days once in a day and hair length, serum total protein, and total testosterone were measured. RESULTS: Our formulations show increase in hair growth and serum total protein at concentration dependent manner with effect to standard and control groups. Serum total testosterone decreases according to a concentration dependent manner. CONCLUSION: Further, series of investigations are, however, necessary to remain exploration, which includes their structural elucidation, characterization, clinical safety, reliability and molecular mechanism involved in this pharmacological activity.

Antinociceptive activity of aqueous extract of Pachyptera hymenaea (DC.) in mice.

The standardized aqueous extract of leaves of Pachyptera hymenaea (DC.) belonging to family Bignoniaceae was investigated for possible antinociceptive effect in mice. Three different models were used to study the effects of extract on nociception, namely acetic acid-induced writhing test, formalin test (paw licking test) and tail flick test in mice. The extract was administered 1h prior to pain induction in the dose range of 25, 50 and 75mg/kg orally. The extract at the given dose range reduced the acetic acid induced nociception by 44.03, 52.90 and 62.46% respectively. The extract reduced formalin effect in both the phases of experiment by 32.36, 41.94, 54.29% and 35.39, 50.17, 55.86% respectively. In the tail flick study, animals' reaction time were increased by 22.69, 38.24 and 40.26% at the above selected doses respectively at 120min after drug administration. Naloxone (2mg/kg; s.c.) significantly antagonized the effect of extract in formalin and tail flick method, while partially antagonized the effect in writhing test. However caffeine completely reverted the extract effect in both the phases of formalin test. Results of these studies revealed that the extract have significant antinociceptive activity in the used models with a possible involvement of central mechanism and adenosine system.

Phytochemical investigation and evaluation of anti-inflammatory and anti-arthritic activities of essential oil of Strobilanthus ixiocephala Benth.

Column chromatographic fractionation of essential oil obtained by hydrodistillation from the flowering tops of S. ixiocephala resulted in the isolation of beta-caryophyllene, fenchyl acetate, T-cadinol and a new sesquiterpene alcohol for which a name ixiocephol has been proposed. The beta-caryophyllene and fenchyl acetate were identified by Co-TLC with authentic samples whereas T-cadinol and ixiocephol were structurally elucidated by UV, IR, 1H NMR, 13C NMR and Mass spectral data. The GC-MS analysis of the essential oil has also revealed the presence of various monoterpenoids and sesquiterpenoids. The essential oil of S. ixiocephala demonstrated a dose dependant anti-inflammatory activity in carrageenan-induced rat paw oedema. It has also revealed good activity in cotton pellet granuloma and adjuvant induced arthritis model in rats.