Griseofulvin is an antifungal drug and is available as oral dosage forms. Development of topical treatment could be advantageous for superficial fungal infections of the skin. In this study, films prepared from the incorporation of griseofulvin-loaded liposomes in chitosan film for topical drug delivery in superficial fungal infections. The properties of the films were characterized regarding mechanical properties, swelling, ability to transmit vapor, drug release, thermal behavior, and antifungal efficacy against Microsporum gypseum and Epidermophyton floccosum. The presence of liposomes led to decreased mechanical properties but lower swelling ratio. Higher amount of drug permeation and rate of flux were obtained by liposomes incorporated in films compared to liposomal formulations. Antifungal efficacy of formulations was confirmed against two species of dermatophytes in vitro. Therefore, two concepts of using vesicular carrier systems and biopolymeric films have been combined and this topical novel composite film has the potential for griseofulvin delivery to superficial fungal infections.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

The aim of this research is to prepare and characterize solid dispersion of efavirenz – polyvinylpyrrolidone (PVP) K-30 by freeze drying to increase its solubility. Solid dispersion of efavirenz – PVP K-30 was prepared by solvent evaporation method with ratio 2:1, 1:1, and 1:2 and dried using a freeze dryer. Characterizations were done by scanning electron microscopy (SEM), powder X-ray diffraction analysis, differential thermal analysis (DTA), and Fourier transform infrared (FT-IR) spectroscopy. Solubility test was carried out in CO₂-free distilled water, and efavirenz assay was conducted using high-performance liquid chromatography with acetonitrile:acetic acid (80:20) as the mobile phases. Powder X-ray diffractogram showed a decrease in the peak intensity, which indicated the crystalline altered to amorphous phase. DTA thermal analysis showed a decrease in the melting point of the solid dispersion compared to intact efavirenz. SEM results indicated the changes in the morphology of the crystal into an amorphous form compared to pure components. FT-IR spectroscopy analysis showed a shift wavenumber of the spectrum efavirenz and PVP K-30. The solubility of solid dispersion at ratio 2:1, 1:1, and 1:2 was 6.777 μg/mL, 6.936 μg/mL, and 14,672 μg/mL, respectively, whereas the solubility of intact efavirenz was 0.250 μg/mL. In conclusion, the solubility of solid dispersion increased significantly (P < 0.05).

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

[FULL TEXT]  [PDF]  [Mobile Full text]  [EPub]  [PubMed]

Resveratrol is a naturally occurring polyphenol, possesses several pharmacological activities including anticancer, antioxidant, antidiabetic, antinociceptive, and antiasthmatic activity. Little is known about its hepatoprotective action mechanisms. This study was conceived to explore the possible protective mechanisms of resveratrol compared with the hepatoprotective silymarin in thioacetamide (TAA)-induced hepatic injury in rats. Thirty-two rats were equally divided into four groups; normal control (i), TAA (100 mg/kg) (ii), TAA + silymarin (50 mg/kg) (iii), and TAA + resveratrol (10 mg/kg) (iv). Liver function and histopathology, pro-inflammatory cytokines, oxidative stress, and apoptotic markers were examined. Data were analyzed using ANOVA test followed by Tukey post hoc test. Compared to TAA-intoxicated group, resveratrol mitigated liver damage, and inflammation as noted by less inflammatory infiltration, hydropic degeneration with decreased levels of tumor necrosis factor-alpha, interleukin-6, and interferon-gamma by 78.83, 18.12, and 64.49%, respectively. Furthermore, it reduced (P < 0.05) alanine and aspartate aminotransferases by 36.64 and 48.09%, respectively, restored hepatic glutathione content and normalized superoxide dismutase and malondialdehyde levels. While it inhibited nuclear factor-kappa B, cytochrome 2E1, and enhanced apoptosis of necrotic hepatocytes via increasing caspase-3 activity. Our findings indicated that the potential hepatoprotective mechanisms of resveratrol are associated with inhibition of inflammation, enhancing the apoptosis of necrotic hepatocytes, and suppression of oxidative stress.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

The aim of this study was to investigate the influence of absorption enhancers in the uptake of hydrophilic compounds. The permeation of the two hydrophilic drug models gentamicin and 5 (6)-carboxyfluorescein (CF) across the brush border membrane vesicles and Caco-2 cell lines were evaluated using total saponins of Acanthophyllum squarrosum, Quillaja saponaria, sodium lauryl sulfate, sodium glycocholate, sodium taurodeoxycholate , and Tween 20 as absorption enhancers. Transepithelial electrical resistance (TEER) measurement was utilized to assess the paracellular permeability of cell lines. Confocal laser scanning microscopy (CLSM) was performed to obtain images of the distribution of CF in Caco-2 cells. These compounds were able to loosen tight junctions, thus increasing paracellular permeability. CLSM confirmed the effect of these absorption enhancers on CF transport across Caco-2 lines and increased the Caco-2 permeability via transcellular route. It was also confirmed that the decrease in TEER was transient and reversible after removal of permeation enhancers.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Considering the importance of accreditation for hospital pharmacies, this study was to determine the challenges of medication management in hospital pharmacies affiliated with Shiraz University of Medical Sciences, Iran. The study was a mix-method research conducted in two qualitative and quantitative phases during the years 2014–2015 in Shiraz, Iran. National Accreditation Standard checklist for hospitals was used for data collection in the first phase, and Delphi method was applied in three rounds to achieve the most challenges of medication management and the related solutions. Results indicated a medium status of accreditation for all three dimensions in the above hospital pharmacies (3.53, 42.15 and 7, respectively). Lack of clinical pharmacists, nonparticipation of the pharmacy director in annual budgeting, lack of access to patient information, discontinuity of pharmaceutical care for patients discharged, defects in pharmacy staff training, lack of legislation in support of pharmacists and lack of adequate access to physicians' prescriptions, shortages in reporting medication errors, and lack of evidence related to microbial contamination are the most challenges extracted from the second phase. It seems that the studied hospital pharmacies encounter numerous problems regarding accreditation, pharmaceutical care as well as appropriate medication management and supply chain. Attempts to solve these problems can play an important role in improving the efficiency and effectiveness of pharmacies in Iran.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Categorized as a Biopharmaceutics Classification System Class II drugs, atorvastatin (ATV) exhibits low aqueous solubility and bioavailability thus presenting an obstacle and great challenge to formulation researchers. Numerous studies are available in regard to the solubility enhancement of ATV, but very few actually describe this phenomenon in terms of thermodynamics and the solute-solvent interaction. Arginine (ARG) is an amino acid that has been reported to enhance the solubility of the highly insoluble wheat protein gluten through hydrogen bonding and π electron-cation interaction. To our knowledge, ARG has never been investigated as a solubility enhancement agent of aqueous insoluble drugs. Thus, this study aimed to elucidate the solute-solvent and solute-cosolute interactions and derive thermodynamic parameters that bolstered the solubility of ATV in the presence of ARG. We examined the electrolytic conductance and densities of ATV-ARG binary system covering the temperature ranging from 298.15 K to 313.15 K. Conductometric and volumetric parameters such as limiting molar conductance, association constants, limiting partial molar volumes, and expansibility values were calculated. Additionally, thermodynamic parameters (ΔG⁰, ΔH⁰, ΔS⁰, and E_s) involved in the association process of the solute in the aqueous solution of ARG were also determined.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Therapeutic properties of fungal metabolites and silver nanoparticles have been well documented. While fungal metabolites have been used for centuries as medicinal drugs, potential of biogenic silver nanoparticles has recently received attention. We have evaluated the antimicrobial potential of Aspergillus terreus crude extract, silver nanoparticles and an amalgamation of both against four pathogenic bacterial strains. Antimicrobial activity of the following was evaluated – A. terreus extract, biogenic silver nanoparticles, and a mixture containing extract and nanoparticles. Four pathogenic bacteria - Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, and Bacillus cereus were used as test organisms. Phenol, flavonoid, and alkaloid content of extract were determined to understand the chemical profile of the fungus. The extract contained significantly high amounts of phenols, flavonoids, and alkaloids. The extract and biogenic silver nanoparticle exhibited significant antibacterial activity at concentrations of 10 μg/ml and 1 μg/ml, respectively. When used in combination, the extract-nanoparticle mixture showed equally potent antibacterial activity at a much lower concentration of 2.5 μg/ml extract + 0.5 μg/ml nanoparticle. Given its high antibacterial potential, the fungal extract can be a promising source of novel drug lead compounds. The extract – silver nanoparticle mixture exhibited synergism in their antibacterial efficacy. This property can be further used to formulate new age drugs.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

In view of the toxicity of chromium (Cr³⁺) ions, it was explored the damaging effects that this ion could induce in cell membranes. The measurement of the effects induced by Cr³⁺ ions on electrophysiological parameters of short-circuit current and on the potential difference were investigated using the outer side (mucosal) and the inner side (serosal) of toad Pleurodema thaul skin. The results showed a decreased on electrophysiological parameters when it were administered concentrations of 33, 100 and 200 μM of Cr³⁺, the results also suggest that the administration of Cr³⁺ inhibits the ion transport in toad skin by the interaction of Cr³⁺ with lipid bilayers or protein constituents of membrane, and not by an inhibition of the active transport of ions across Na⁺ channels.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

[FULL TEXT]  [PDF]  [Mobile Full text]  [EPub]  [PubMed]