Pharmaceutical Sciences
Volume:14 Issue: 2, 2008

Possible serotonergic modulation of acute peripheral inflammation was investigated in rat adopting air pouch as an experimental model. Air pouch type carrageenan-induced inflammation model on the back of the male Wistar rats was used. Injection of carrageenan solution into an air pouch induced gradual increases in the pouch fluid volume and leukocytes accumulation in the pouch exudates as well as granulation tissue weight. Granisetron (12.5, 25, 50, 100, 200, 400 & 800μg) was injected at the same time as the carrageenan. Granisetron (50, 100 & 200, 400 μg) was found to inhibit the number of white cells in the exudates at 6 hours after the carrageenan injection significantly (from 119.6 ± 7.8 million in control group to 62.5 ± 6.7 million, 69.5 ± 9.8 million, 82.5 ± 4.8 million and 86.3± 6.3 million respectively). The pouches fluid volumes were decreased significantly by doses of 12.5μg (3.6± 0.1ml), 25μg (3.4 ± 0.1ml), 100μg (3.6 ± 0.2 ml), 400μg (3.7 ± 0.1ml), 800μg (3.6 ± 0.1ml) of granisetron compare to control (4.1 ± 0.08ml). Tissues weight at 6 hr after carrageenan injection was increased by doses of 12.5 μg (5.04 ± 0.6 g), 25 μg (3.06 ± 0.5 g) and 800 μg (. ± 0.2 g) and was decreased with 100 μg granisetron (1.3 ± 0.2 g) significantly compare to control group (5.04 ± 0.6 g). The study confirms that the serotonergic system is capable of modulating peripheral inflammation via 5HT3 receptors.

The aim of this study was evaluation of the effect of complexation of with β cyclodextrine (CDX) on transdermal absorption of oxybenzone and formulation of a sunscreen product with low transdermal absorption using this technique. In the first step, we designed a base for our formulation with suitable features in the case of appearance, viscosity and stability (including physical and chemical stability). Sunscreen-CDX Complexes were prepared by different methods including: Kneading, cogrinding and solvent evaporation. The performance of complexation process was assessed by DSC and FTIR spectra and coevaporetion method was selected as the best complexation technique. Transdermal absorption studies were carried out on the base formulations with sunscreen, sunscreen plus CDX as simple physical mixture and sunscreen-CDX complexes. Transdermal studies were done using full thickness skin of wistar rats and Standard Franz diffusion cell equipment. Sunscreen in the samples taken from receptor phase of diffusion cells were analyzed by HPLC method. Results showed that complexation with CDX can significantly decrease flux of sunscreen agent (14.5 fold lower than formulation without CDX) whereas formulation containing sunscreen-CDX physical mixture did not showed significant decrease in flux compared with CDX free formulation. (0.4477 and 0.3575μg/cm2/h for formulation of sunscreen-CDX simple physical mixture and CDX free formulation respectively). Lag time of skin penetration also significantly increased with CDX in formulations containing sunscreen-CDX complex (2.53 and 1.88h for formulations containing sunscreen-CDX complex and CDX free formulations respectively). these results demonstrated the complexation with CDX can improve characteristics of sunscreen formulation prepared with Eusolex 4360 active ingredient significantly.

Propofol is an ultra short acting intravenous anesthetic used for induction and maintenance of anesthesia and it can also be used for sedation purposes. Pain on injection is one of the main disadvantages of propofol and a common problem during induction of anesthesia. The use of lidocaine was found to be an effective prevention of injection pain. The primary objective of this study was to investigate the effect of remifentanil on the incidence and severity of pain during injection of propofol in comparison with lidocaine. In a randomised, double-blind study we compared the efficacy of continuous remifentanil infusion (0.25 μg.kg-1 min-1) with 40 mg lidocaine and placebo in the prvention of injection pain due to intravenous propofol administration (2 mg/kg) in 90 patients scheduled for elective surgery. Pain severity was evaluated using a four-point scale. The incidence of injection pain was 73% in the placebo group and could be reduced significantly by using lidocaine (27%; p < 0.0015) or remifentanil (30%; p < 0.005). Analysis of the pain scores showed a significant difference between remifentanil and placebo (p < 0.00002) as well as between lidocaine and placebo (p < 0.0005). There was no significant difference between remifentanil and lidocaine. Remifentanil provided effective pain relief, comparable with lidocaine, and is an alternative as part of an intravenous anaesthesia regimen to using another concomitant drug.

Development of azole resistance in opportunistic fungi is the most problematic reason in immunocompromised patients and at present time, there is an increased awareness of the morbidity and mortality associated with fungal infections caused by resistant fungi to imidazole. This research was carried out for cloning and sequencing of Fluconazole resistance gene. Using genomic DNA of Aspergilus fumigatus (ATCC strain 90254) a primary 800 bp PCR product and then a secondary 1750 bp inverse PCR product were obtained. The 1750 bp PCR product was gel purified and cloned into E. coli using the suitable plasmid. Plasmid was extracted from transformed E. coli and the presence of expected insert into plasmid, was confirmed by digestion of plasmid using Eco R1 restriction enzyme. Also southern analysis using standard protocol was carried out for investigation of gene expression. Gel purified 1750 bp band was sequenced and after deletion of extra nucleotides from both side of residue a 1703 bp motif submitted at NCBI gene bank with accession No.: A 848856. In conclusion considering (resistant to fluconazole) A. fumigatus resistance gene to this compound was cloned and sequenced successfully in our lab. Since A. fumigatus is increasingly resistant to the widely used fluconazole, we emphasize for future additional studies for expression of this gene and its mRNA transcription to understand the effective and inhibitor factors for expression of gene.

Crystallization is often employed for purifying a drug substance in pharmaceutical industry and, in addition, plays an important role in defining the stability and drug release properties of the final dosage forms. Advances of chemical synthesis have achieved control over drug identity and purity, but control over the physical form and crystallinity remains poor. It should be considered that even minor change in crystallization condition can produce significant change in the crystal and powder physical properties such as particle size, shape, and defect structure. These effects have been recognized as the major batch-to-batch and source variation problems leading to inconsistency of the final dosage forms properties. The purpose of this review is to indicate the importance of physical properties of the crystals and their roles in the performance of dosage forms.

Erica arborea L. (EA, Ericaceae) is a topical shrub or small tree predominantly found in all around the Mediterranean area such as Çanakkale, Turkey, which is used traditionally as a diuretic, urinary antiseptic, anorexiant and against constipation. However, its other pharmacological effects have not been yet elucidated clearly. The aim of this study was to investigate the analgesic effect of its hydroalcoholic-extract on hot plate test, as a model of thermal acute pain. Study was carried out on male Swiss mice weighing 30-35 g. In order to study acute pain, hot plate test with set point 50±1 °C and cut off time 50 Sec was used. Methanolic extract of aerial parts was prepared by maceration method and then its analgesic effect was studied at the doses of 10, 20 and 30 mg/kg, i.p. In addition, the methanolic fractions of 20, 40, 60, 80 and 100% were prepared by solid phase extraction method, and then their analgesic effect was investigated at the dose of 5 mg/kg, i.p. The effect of methanolic extract and fractions were compared with the analgesic effect of morphine (10 mg/kg, i.p.) as a standard analgesic drug. Results obtained from this study showed that methanolic extract of EA had analgesic effect (P<0.05) at the dose of 10 mg/kg, i.p. The analgesic effect of extract was less than (P<0.05) morphine 10 mg/kg, i.p.). Among the prepared-methanolic fractions, only the fraction 20% (10 mg/kg, i.p.) caused significant (P<0.05) analgesia. Moreover, the methanolic extract (10 mg/kg, i.p.) has not any motor deficit effect in rotarod test. We conclude that total methanolic extract and faction 20% of EA have a good pain relief effect in hot plate test. The analgesic effect of EA was also comparable to that of morphine, as a well known analgesic drug. In order to relate the analgesic effect of EA to particular phytochemicals, further investigations should be done.

Spectrophotometric methods are amongst the most important methods used for determination of encapsulated proteins in particulate drug delivery systems. In Bradford method, which is used frequently, some interfering agents could affect the precise determination of proteins. In such a conditions, other methods with less interactions, such as spectrofluorimetry, can be used. Tetanus toxoid (TT) was conjugated with fluorceinisothiocianate (FITC), as a fluorescent agent. Buffer salts and unconjugated FITC were separated by dialysis and ultrafiltration. Alginate microspheres and liposomes encapsulated with fluorescent TT were prepared by emulsification-internal phase gelation and solvent evaporation, respectively. encapsulated TT in microspheres and liposomes was determined by Bradford and spectroflourimetric methods. Mean encapsulation efficiency of FITC-TT in microspheres was obtained to be 38.33 ± 6.11 and 21.33 ± 2.1, by Bradford and fluorimetry methods, respectively (P<0.01). In Bradford method, the blank microspheres showed high absorbances which could be caused by interaction from sodium alginate polymer. But in the fluorimetric method the blank microspheres showed little absorbances, so this method is more reliable. Mean encapsulation efficiency of FITC-TT in liposomes was determined by indirect method, as 46.33 ± 6.23 and 56 ± 3, by Bradford and fluorimetry methods (P<0.05). In Bradford method, supernatant of blank liposomes showed high absorbances which could be rooted from interaction of free lipids. But in the fluorimetry method supernatant of the blank liposomes showed little emission, so this method is more reliable. In determination of encapsulation efficiencies of proteins in microspheres and liposomes, when spectrophotometric methods due to interfering agents, could not be utilized precisely, spectrofluorimetric method can be preferred.