A nanocomposite competent to overcome solubility and permeation issues of capsaicin and thiocolchicoside simultaneously in gout management: Fabrication of nanocubosomes.

This study aimed to formulate nano-cubosomes (NCs) co-loaded with capsaicin (CAP) and thiocolchicoside (TCS) to enhance their bioavailability and minimize associated potential side effects through transdermal delivery alongside their synergistic activity. Twenty seven (27) nano-cubosomal dispersions were prepared according to Box-Behnken factorial design and the effect of CAP, TCS, glyceryl mono oleate (GMO) and poloxamer 407 (P407) concentrations on particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency were assessed. The results revealed that the optimized formulation exhibited a mean droplet size of 503 ± 10.3 nm, PDI of 0.405 ± 0.02, zeta potential of -10.0 ± 1.70 mV and entrapment efficiency of 86.9 ± 3.56 %. The in vivo anti-inflammatory effect of optimized formulation was studied in rats by injecting carrageenan to induce edema. The results of in vivo study showed that transdermal application of nano-cubosomes co-loaded with CAP and TCS significantly (p value < 0.05) improved carrageenan induced inflammation compared with standard treatment. The analgesic activity of optimized formulation was evaluated in rats by using Eddy's hot plate method. The findings of analgesic activity illustrated that the analgesic effects exhibited by test formulation may be associated with increased licking period and inhibition of prostaglandins level. In conclusion, the transdermal application of NCs co-loaded with CAP and TCS may be a promising delivery system for enhancing their bioavailability as well as synergistic analgesic and anti-inflammatory activity in gout management.

Formulation and Evaluation of Topical Linezolid Nanoemulsion for Open Incision Wound in Diabetic Animal Model.

The present study aimed to investigate the role of topical nanoemulsion of linezolid in attenuating diabetic wound by delivering the drug to the target tissue. The nanoemulsions (NEs) were prepared by high-pressure homogenization and subjected to thermodynamic stability, pH, droplet size, viscosity, surface charge, polydispersity index (PDI), entrapment efficiency, drug content, and in vitro drug release. All formulations were thermodynamically stable. The pH was in the range of 5 to 6. The viscosities of LZD-0, LZD-1, LZD-2, and LZD-3 were recorded as 68.75 ± 2.23 mPas, 69.56 ± 2.11 mPas, 96.45 ± 3.39 mPas, and 45.5 ± 1.12 mPas respectively. LZD-1 exhibited droplet size of 376.5 nm ± 0.98, surface charge - 22.5mV, and PDI 0.387. Drug content and entrapment efficiency of LZD-1 were found to be 93 ± 3.31 % and 72 ± 1.67 %, respectively. LZD-1 released 80 ± 2.87% of drug. Due to significant (P < 0.05) in vitro results, LZD-1 formulation was selected for in vivo evaluation. Diabetes was induced in Sprague-Dawley rats using intraperitoneal streptozotocin injection at dose of 50 mg/kg. Open-incision wounds were inflicted among all diabetic rats at dorsal shaved area. Randomly, all rats were divided into positive control (blank formulation), negative control (no formulation), and test group (LZD-1). Wound healing occurred in order of test group > positive control > negative control. Skin histology and tensile strength also revealed significant results. The study concluded that topical nanoemulsion of linezolid may open new horizon in treating diabetic wounds.

Pharmacological effects (gastrointestinal, respiratory and vascular) of Calligonum polygonoides: Animal model based studies.

The aim of this study was to analyze gastrointestinal, respiratory and vascular pharmacological effects of 70% hydro-alcoholic extract of Calligonum polygonoides (Cp. Cr) in animal models. All the procedures were carried-out as per previous literature with slight modification where necessary. It was found that Cp. Cr affected significant relaxation of spontaneous and K+ (80 mM) induced contractions. The results showed a corresponding shift of calcium concentration response curves. Similarly Cp. Cr showed relaxant effect on trachea in carbachol (Cch) induced tracheal contractions. Moreover, contractions induced by phenylephrine (1µM) in quarantine rabbit aortic preparations causes Cp. Cr induced relaxation of aortal contractions. Verapamil was used as a standard calcium channel blocker. The findings of this study suggested vasodilator, bronchodilator and spasmolytic effects of Cp. Cr.

Marine Algae-Derived Bioactive Compounds: A New Wave of Nanodrugs?

Marine algae are rich in bioactive nutraceuticals (e.g., carbohydrates, proteins, minerals, fatty acids, antioxidants, and pigments). Biotic (e.g., plants, microorganisms) and abiotic factors (e.g., temperature, pH, salinity, light intensity) contribute to the production of primary and secondary metabolites by algae. Easy, profitable, and sustainable recovery methods include novel solid-liquid and liquid-liquid extraction techniques (e.g., supercritical, high pressure, microwave, ultrasound, enzymatic). The spectacular findings of algal-mediated synthesis of nanotheranostics has attracted further interest because of the availability of microalgae-based natural bioactive therapeutic compounds and the cost-effective commercialization of stable microalgal drugs. Algal extracts can serve as stabilizing/capping and reducing agents for the synthesis of thermodynamically stable nanoparticles (NPs). Different types of nanotherapeutics have been synthesized using physical, chemical, and biological methods. Marine algae are a fascinating source of lead theranostics compounds, and the development of nanotheranostics has been linked to enhanced drug efficacy and safety. Indeed, algae are remarkable nanobiofactories, and their pragmatic properties reside in their (i) ease of handling; (ii) capacity to absorb/accumulate inorganic metallic ions; (iii) cost-effectiveness; and (iv) capacity of eco-friendly, rapid, and healthier synthesis of NPs. Preclinical and clinical trials shall enable to really define effective algal-based nanotherapies. This review aims to provide an overview of the main algal compounds that are nutraceuticals and that can be extracted and purified for nanotheranostic purposes.

Anti-inflammatory and anti-nociceptive activities of polyphenols from Feijoa fruit and leaves.

Many pharmacological activities have been reported from plants polyphenols. The aim of this study was to investigate anti inflammatory and antinociceptive activities of polyphenols from Feijoa sellowiana fruit and leaves. For the anti-inflammatory activity evaluation, inhibition of carrageenan induced edema was used. While for the evaluation of antinociceptive activity of the extract, writhing and hot plate tests in mice were used. Impairment in mouse coordination was evaluated by rota-rode test. Carrageenan induced edema was significantly inhibited by the extract at 50-400 mg kg-1 doses, when comparison was made with control group. The extract of leaf at the dose of 50 mg kg-1 i.p. the activity was equipotent with diclofenac (p>0.05). Extract reduced the writhing count in 50-400 mg kg-1 of doses. Fruit extract showed higher activity than diclofenac (p<0.001) at 400 mg kg-1 doses. In all tested doses, the extract significantly augmented the pain threshold in hot plate thermal test. No locomotor impairment in mice was induced by the extract at any tested doses. Extract was safe and didnot demonstrate any noxiousness up to 1 g kg-1 .This study indicates the potential therapeutic use of Feijoa as a potent anti-inflammatory and antinociceptive agent.

Piroxicam loaded polymer hybrid microspheres based tablets with modified release kinetics: Development, characterization and in vivo evaluation.

Piroxicam (PC) is a non-steroidal anti-inflammatory drug characterized by poor aqueous solubility and reported to cause and impart crucial GIT irritation, bleeding, peptic and duodenal ulcer. Engineering of PC loaded microcapsules and its surface modification using different polymers has become the popular approach to address the said issues. The purpose of the study was to develop new PC loaded gastro-protective polymer hybrid microspheres (PHM) with subsequent conversion to tablet dosage form having modified dissolution rate and improved bioavailability. The crystallinity of the PC loaded PHM were established through powder X-ray diffraction. The optimised microspheres, PC-M1 with particle size 32±3.0µm, entrapment efficiency 83.78±2.5% and in vitro drug release 87.1±2.6% were further subjected to tablets development and in vivo evaluation. The in vitro drug release study conducted for PHM at pH media 1.2 and 6.8 demonstrated retarded and enhanced drug release rates (P<0.001) respectively. Both accelerated and real time stability studies confirmed stability of the PC loaded PHM based tablets. A substantial improvement in the drug plasma concentration 12.6±2.36 (P<0.001) was observed for the produced tablets compared to the marketed formulations.

Ecological and Industrial Implications of Dynamic Seaweed-Associated Microbiota Interactions.

Seaweeds are broadly distributed and represent an important source of secondary metabolites (e.g., halogenated compounds, polyphenols) eliciting various pharmacological activities and playing a relevant ecological role in the anti-epibiosis. Importantly, host (as known as basibiont such as algae)-microbe (as known as epibiont such as bacteria) interaction (as known as halobiont) is a driving force for coevolution in the marine environment. Nevertheless, halobionts may be fundamental (harmless) or detrimental (harmful) to the functioning of the host. In addition to biotic factors, abiotic factors (e.g., pH, salinity, temperature, nutrients) regulate halobionts. Spatiotemporal and functional exploration of such dynamic interactions appear crucial. Indeed, environmental stress in a constantly changing ocean may disturb complex mutualistic relations, through mechanisms involving host chemical defense strategies (e.g., secretion of secondary metabolites and antifouling chemicals by quorum sensing). It is worth mentioning that many of bioactive compounds, such as terpenoids, previously attributed to macroalgae are in fact produced or metabolized by their associated microorganisms (e.g., bacteria, fungi, viruses, parasites). Eventually, recent metagenomics analyses suggest that microbes may have acquired seaweed associated genes because of increased seaweed in diets. This article retrospectively reviews pertinent studies on the spatiotemporal and functional seaweed-associated microbiota interactions which can lead to the production of bioactive compounds with high antifouling, theranostic, and biotechnological potential.

Fabrication, Physical Characterizations, and In Vitro, In Vivo Evaluation of Ginger Extract-Loaded Gelatin/Poly(Vinyl Alcohol) Hydrogel Films Against Burn Wound Healing in Animal Model.

Crude ginger has been used to treat wounds since ancient times till nowadays. The present study aimed at designing and characterizing topical hydrogel films loaded with ginger extract for wound healing in animal model. The hydrogel films were prepared using PVA and gelatin. The prepared films were evaluated for FTIR analysis, surface morphology, pH, swelling behavior, in vitro release, and % drug content. The wound-healing activity of the extract-loaded hydrogel films was compared with commercially available Silver Sulfadiazine® cream. The drug was compatible with the selected polymers and indicated the suitability of the selected polymers for preparation of topical hydrogel films. The SEM images clearly indicated porous structure of the prepared hydrogel films. Slight changes were observed in pH, ranging from 4.98 ± 0.079 in the beginning of the study to 4.9 ± 0.58 in the end. The swelling percentage after 8 h was 257.7%. The films released 78.7 ± 1.7% of the drug in 250 min. The percent drug content was 97.78 ± 5% which did not change significantly during the storage period. The hydrogel films showed similar wound-healing activity as compared to the commercial product (p > 0.05; ANOVA), while greater wound-healing activity as compared to the control group (p < 0.05; ANOVA) evidenced by intensive collagen formation in histopathological analysis.

Formulation Development, Characterization, and Evaluation of a Novel Dexibuprofen-Capsaicin Skin Emulgel with Improved In Vivo Anti-inflammatory and Analgesic Effects.

Transdermal application of analgesics allows efficient and painless delivery of medication with minimum side effect. This study was designed with the aim to formulate and characterize dexibuprofen-capsaicin emulgel for transdermal drug delivery with improved anti-inflammatory and analgesic effects. The emulgel was prepared and evaluated for physical examination, stability, spreadability, rheological behavior, viscosity, drug content determination, FTIR analysis, and ex vivo studies. Anti-inflammatory (carrageenan-induced paw edema) and analgesic (hot plate latency test) effects were determined in Sprague-Dawley rats. The dexibuprofen-capsaicin emulgel showed good physical appearance and stability having average pH 5.5 to 6.0, conductivity 73-76 s/m, spreadability (12-)17 g cm/s, drug content 102.84% ± 0.53 (for capsaicin) and 94.09% ± 0.41 (for dexibuprofen), and FTIR compatibility. It was noted that 86.956% ± 1.46 (with 100 mg menthol), 76.687% ± 1.21 (75 mg menthol), and 65.543% ± 1.71 (without menthol) of capsaicin were released. Similarly 81.342% ± 1.21 (with 100 mg menthol), 72.321% ± 1.31 (75 mg menthol), and 52.462% ± 1.23 (without menthol) of dexibuprofen were released. The cumulative amount of capsaicin permeated through rabbit skin was 9.83 ± 0.037 µg/cm2 with 100 mg menthol (as permeation enhancer), 7.23 ± 0.037 µg/cm2 with 75 mg menthol, and 2.23 ± 0.061 µg/cm2 without menthol after 6.5 h. The permeation of dexibuprofen was 19.53 ± 0.054 µg/cm2, 13.87 ± 0.032 µg/cm2, and 3.83 ± 0.074 µg/cm2. Carrageenan-induced paw edema of rat was effectively inhibited by the optimized emulgel. Similarly it was observed that DCE5 shows higher analgesic activity compared with marketed diclofenac sodium emulgel (Dicloran®). The conclusion of this research study evidently indicated a promising synergistic potential of dexibuprofen-capsaicin emulgel as an alternative to the conventional topical dosage form.

Development, characterization and evaluation of ginger extract loaded microemulsion: In vitro and Ex vivo release studies.

Zingeber officinale (ginger) has been used for a long time in conventional medicine for the management of many diseases most important of which is inflammatory diseases. The aim of this study was formulation of topical microemulsion system to enhance the solubility, stability and release profile of ginger extract, as it is unstable in the presence of light, air, heat and long term storage. The solubility of ginger extract in different oils, surfactants, and cosurfactants was determined in order to find the optimal components for microemulsion. Isopropyl myristate (IPM) was selected as oil phase, tween 80 and PEG 400 were selected as surfactant and co-surfactant respectively based on highest solubility values. Pseudo-ternary phase diagram was constructed in order to find out the microemulsion region. The prepared microemulsions were evaluated for pH, viscosity, conductivity, refractive index, globular size, zeta potential, polydispersity index, ginger extract content, in-vitro and ex-vivo release profiles. The formulation GE1 showed best physicochemical properties with smallest globular size (19.75nm), highest release rate and flux value. It also showed significant (p<0.05) anti-inflammatory effect as compared to reference piroxicam drug solution. It is concluded that ginger extract can be used to develop stable microemulsion system with better skin permeation and promising antiinflammatory activity.

Antibacterial and antibiofilm properties of traditional medicinal plant from Sheikh Buddin range.

During current project, antibacterial and antibiofilm properties of traditional medicinal plant Ziziphus nummularia leaf extract and various fractions was investigated. The plant leaves were dried and extracted using 90% methanol followed by sequential fractionation using liquid-liquid fractionation. The fractions of a diverse polarity including chloroform, n-hexane, methanol and ethyl acetate and aqueous extracts were obtained that was further analysed by using HPLC. The phytochemical screening indicated presence of saponins, triterpenes and flavonoids. During DPPH assay, the methanolic fraction presented highest activity (IC50 193.1µg/mL), followed by ethyl acetate (IC50 220µg/mL) and chloroform (IC50 263µg/mL) fractions respectively. During FRAP assay, FRAP value for Z. nummularia extract 20.43µM. Among fractions, ethyl acetate fraction presented highest FRAP value (370.2µM), followed by chloroform (204µM) and methanolic (249µM) fractions. The antimicrobial activity of chloroform fraction was significantly high against P. aureginosa (6mm), L. monocytogenes, S. aureus (5mm), K. pneumoniae, B. Subtillus and E. coli (4mm). The ethyl acetate part presented significant activity (MIC 4mg/mL) against S. aureus, B. Subtillus and L. monocytogenes. The total extract and fractions were further tested for MBC and the MBC for ethyl acetate fractions was 4mg/mL, whereas all other fractions exhibited MBC >10mg/mL. No activity was recorded against Aspergillus niger. During antibiofilm assay, n-hexane fraction presented highest inhibition (88%) followed by ethyl acetate (69%) chloroform (65%) fractions. It was concluded that Z. nummularia possess moderate antimicrobial and antibiofilm activities. Further a synergistic effect is suggested in formulation having Z. nummularia.

Development, characterization and evaluation of in-vitro anti-inflammatory activity of ginger extract based micro emulsion.

Zingeber officinale is a commonly used plant which has been shown to possess anti-inflammatory activity. The active compounds present in ginger are gingerols, shagaols and paradol. The aim of this study was formulation of topical microemulsion system to enhance the solubility and stability of ginger extract, as it is unstable in the presence of light, air, heat and long term storage, and to evaluate its anti-inflammatory activity. The solubility of ginger extract in different oils, surfactants, and co-surfactants was determined in order to find the optimal components for microemulsion. IPM was selected as oil phase, tween 80 and PEG 400 were selected as surfactant and co-surfactant respectively based on highest solubility values. Pseudo-ternary phase diagram was constructed in order to find out the microemulsion region. The prepared microemulsions were evaluated for pH, viscosity, conductivity, refractive index, globular size, zeta potential, polydispersity index, ginger extract content. The formulation F1 showed best physicochemical properties with smallest globular size. It also showed significant (p<0.05) anti-inflammatory effect as compared to reference piroxicam drug solution. Based on the results, it is concluded that ginger extract can be used to develop stable microemulsion system and promising anti-inflammatory activity.

Evaluation of antibiotic resistant bacteria in underground drinking water and transfer of their resistant character to normal flora of the body.

The untreated surface water for drinking and domestic use is an alarming situation to public health especially in prevalence of antibiotics resistant bacteria. This investigation aimed to isolate and identify the antibiotic resistance bacteria in underground water samples in district Dera Ismail Khan, Pakistan. The underground water samples were collected from four different places using hand pumps (Khyber town, riverside, Gomal University and united town). Cultured on nutrient agar media, identified by Gam staining and biochemical tests. There after antibiotic resistance assay were performed by measuring zone of inhibition of different antibiotics by disc diffusion method. Six different bacterial colonies were isolated and identified as Enterobacteriaceae, Serriata specie, Proteues, Pseudomonas, all these bacterial colonies were 33% resistant to chloramphenicol with and 100% resistant to amoxicillin. Some colonies were also considered as resistant, according to the criteria of National Committee for Clinical Records (NCCL) that less than 10mm zone of inhibition are considered as resistant. Subsequently, the chloramphenicol resistance bacteria were analyzed for their ability to transfer resistant gene to sensitive bacteria. In in-vitro method, an isolate M1b (resistant) was found capable to transfer resistance gene to M1a isolate (sensitive) in nutrient rich environment. It was concluded that antibiotics resistance bacteria found in underground water, moreover capable of transferring the antibiotic resistant character to suitable recipient i.e. normal flora of the body or to other pathogens by conjugation.

Synthesis, characterization and evaluation of antibacterial activity of copper oxide nanoparticles against clinical strains of Staphylococcus aureus.

Bacterial resistance is spreading globally due to excessive use of antibiotics, making it one of our times biggest challenges. To address this issue present study was conducted to evaluate the antibacterial activity of copper oxide nanoparticles against methicillin-resistant S. aureus (MRSA). Copper oxide nanoparticles were synthesized by chemical precipitation method and were characterized by UV-Visible, FT-IR spectroscopy, X-ray diffraction (XRD) and Scanning Electron Microscopy. These nanoparticles of 27nm were assessed for antibacterial activity using disc diffusion method. Our results showed superb inhibitory effects of CuO nanoparticles with increase in concentration and complete inhibition was recorded against tested strains of S. aureus at 100µl/ml and 125µl/ml concentration. The study concludes that the drugs which do not show any inhibitory effects against resistant bugs could be augmented with CuO nanoparticles to achieve the treatment goal.

In vitro antifungal activity of 9, 10-dihydrophenanthrene-2-carboxylic acid isolated from a marine bacterium: Pseudomonas putida.

An antifungal compound 9, 10-dihydrophenanthrene - 2 - carboxylic acid was isolated from a marine derived bacterium Pseudomonas putida isolated from surface water samples of Karachi fish harbor coast line. The structure was explored using extensive 1D- and 2D-NMR spectroscopic techniques. The compound was found to be active against fungal strains obtained from clinical samples whereas strong activity was noted against Candida albicans with a MIC value of 20µg/ml, as the purified compound showed promising anticandidal activity a multidisciplinary approach is needed to explore further this compound as potential pharmacological lead compound against Candida spp and will add in the global hunt for clinically functional antifungal agents.

Phytoformulation of Sassurea lappa plant extract: A Single blind, noninvasive and split face study of cream on various skin parameters.

Saussurea lappa (SL) has been reported for its antioxidant and anti-ageing properties. Due to this reason it can be incorporated in a stable phytoformulations for cosmetic use. The objective of the study was to evaluate the anti-aging potential of cosmetic o/w emulsion containing the botanical extract of SL. An emulsion (o/w) was prepared using TEGO® Care 450 (Polyglceryl-3-Methyl Glucose Distearate) emulsifier and final emulsion was loaded with 4 % extract of SL in aqueous phase. This emulsion evaluated for its antioxidant and anti-ageing properties on healthy human subjects using a non-invasive technique called surface evaluation of living skin (SELS). The formulation containing SL extract showed significant (p<0.05) changes in Skin roughness (SEr) as -3.13%, -6.26%, -9.39%; Skin Scaliness (SEsc) as - 4.19%, -8.39%, -12.58%; Skin wrinkles (SEw) as -0.5%, -1.08%, -1.63%; and Skin smoothness (SEsm) as 3.28%, 6.57%, 9.85%, respectively, after 30, 60 and 90 days of continous use. Topical application of the cosmetic cream containing SL extract exerts have a significant anti-aging effects, perhaps due to the presence of Kaempferol, gallic acid, Caffeic acid and other essential phenolics.

Short Communication - Urease inhibitory activity of Hippophae rhamnoids and Cassia fistula.

The rational use of plants as medicine is traced back over five epochs to ancient documents of early civilizations and is certainly as old as mankind. These medicines originally developed from crude drugs like tinctures and tinctures. Minimum 119 chemical substances are derived from 90 plant species and used all over the world as medicines, several of them containing compounds derived from or modelled after naturally occurring lead molecules and 74% of these derived from orthodox medicinal plants. 252 drugs (11%) are believed to be basic and essential by the WHO and are exclusively of plant origin. We have examined anti-urease activity of ethyl alcohol (Et-OH) and methyl alcohol (Me-OH) extracts of H. rhamnoides and Cassia fistula. Berthelot assay was used for the determination of anti-urease activity. The enzyme activity and inhibition was measured through catalytic effects of urease on urea by measuring change in absorbance in the absence and in the presence of inhibitor at 625nm using UV spectrophotometer. In the study, both Et-OH and Me-OH extracts of H. rhamnoides (91.69%±1.21) and C. fisstula (79.44%±0.55) showed stronger action against urease activity. An overview on the medicinal uses of H. rhamnoides and C. fisstula showing anti-urease activity may predict their possible alternative use for stomach problems. This study may help to explain the beneficial effects of these plants against stomach infection associated with pathogenic strains of H. pylori as Urease is the most prominent protein component of H. pylori.

Fabrication of Tamarindus indica seeds extract loaded-cream for photo-aged skin: Visioscan® studies.

INTRODUCTION: Intracellular and extracellular oxidative stress triggered by free radicals promotes skin aging, which is designated by atypical pigmentation and wrinkles. The consumption of antioxidants is an efficacious measure to avert symptoms involved in skin aging. AIM: The current research was commenced to explore the anti-aging potential of antioxidants present in Tamarindus indica seeds extract. MATERIAL AND METHODS: Tamarindus indica seeds extract was obtained by concentrating the ethanolic extract of seeds. The antioxidant activities of the extract were measured by nitric oxide radical scavenging assay, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, hydroxyl radical scavenging assay and superoxide radical scavenging assay. Formulation comprising 4% of the concentrated extract of seeds was formulated by loading it in the internal aqueous phase of water-in-oil (W/O) cosmetic emulsion. The base, used as control, consisted of the same emulsion but without loading Tamarindus indica seeds extract. The cosmetic emulsions were applied to the cheeks of 11 healthy male volunteers for duration of 12 weeks. Both base and formulation were assessed for their antioxidant effects on different skin parameters i.e. skin moisture contents, elasticity and surface evaluation of living skin (SELS). RESULTS: The formulation showed statistically significant (p ≤ 0.05) and the base showed insignificant (p > 0.05) effects on skin elasticity and skin moisture contents. There is a significant decline in SELS, skin scaliness (SEsc), skin wrinkles (SEw), skin smoothness (SEsm), and skin roughness (SEr) parameters after application of the formulation. CONCLUSIONS: Topical application of the cosmetic emulsion entrapped with Tamarindus indica seeds extract containing various antioxidants exerts potential skin antiaging effects.

A stable hydrocortisone nanosuspension for improved dissolution: Preparation, characterization and in vitro evaluation.

Drug nanosuspensions have gained tremendous attraction as a platform in drug delivery. In the present work, a nanosuspension was prepared by a wet milling approach in order to increase saturation solubility and dissolution of the water insoluble drug, hydrocortisone. Size of the generated particeles was 290 nm ± 9 nm having a zeta potential of -1.9 mV ± 0.6 mV. Nanosized particles were found to have a rod shape with a narrow particle size distribution (PDI =0.17). Results of differential scanning calorimetry and X-ray diffraction analyses revealed minor modifications of crystallinity of hydrocortisone following the milling process. Solubility of hydrocortisone was enhanced by nanonization to 875µg/ml ±2.5, an almost 2.9-fold compared to the raw hydrocortisone. Moreover, the nanosuspension formulation substabtially enhanced the dissolution rate of hydrocortisone where >97% of the hydrocortisone was dissolved within 10 minutes opposed to 22.3% for the raw 50% for the raw hydrocortisone and the commercial tablet, respectively. The bioavailability study resulted in AUC 0-9h for HC nanosuspensions (31.50±2.50), which is significantly (p<0.05) higher compared to the AUC 0-9h (14.85±3.25) resulted for HC solution. The nanosuspension was physically stable at room temperature for 24 months.

Essential oils showing in vitro anti MRSA and synergistic activity with penicillin group of antibiotics.

This study was planned in order to investigate effective essential oils to inhibit in-vitro growth of Methicillin resistant Staphylococcus aureus (MRSA). In this study using disc diffusion method anti MRSA activity of ten diverse essential oils extracted from traditional plants namely Thymus vulgaris L, Mentha pulegium, Ocimum sanctum, Mentha piperita, Cymbopogon citratus, Rosmarinus officinalis L., Cortex cinnamom, Citrus nobilis x Citrus deliciosa, Origanum vulgare and Mentha sp. was examined. All the essential oils inhibited growth of S. aureus to different extent, by exhibiting moderate to elevated zones of inhibitions. Essential oils of cinnamon (Cortex cinnamomi) and thyme (Thymus vulgaris L) were observed to be the most powerful against MRSA strains used in this study. At lowest concentration of 25µl/ml essential oils comprehensible zone of inhibition was found 9±0.085mm and 8±0.051mm respectively, and at elevated concentrations there was a total decline in growth of MRSA and a very clear zone of inhibition was observed. A synergistic effect of essential oils in amalgamation with amoxicillin a Penicillin group of antibiotic was also examined. Interestingly a strong synergism was observed with oregano (Origanum vulgare) and pennyroyal mint (Mentha pulegium) essential oils, which were not so effective alone driven out to be important synergistic candidate. Our results demonstrated that essential oils of cinnamon and thyme can be used as potential antimicrobial agent against the Methicillin-resistant Staphylococcus aureus infections and Amoxicillin antibacterial activity can be enhanced using active constituents present in oregano and pennyroyal mint essential oils.