Iranian Journal of Pharmaceutical Research
Volume:6 Issue: 3, Summer 2007

In induction of systemic and mucosal immunity, particulate antigens are more effective than soluble antigens possibly because they are more efficiently endocytosed by mucosal-associated lymphoid tissue (MALT) M cells. In this study, we determined the systemic and mucosal immune responses in rabbits following intranasal immunization of tetanus toxoid TT and CpG-ODN encapsulated within PLGA nanospheres. The mean diameter of (TT) and TT+CpG nanospheres were 753±193 and 684±324 nm, respectively. Encapsulation efficiency of TT and CpG-ODN was determined as 52±7.8% and 30.2±7.4%, respectively. The highest nasal lavage (sIgA) titers were observed in groups immunized with nanosphere formulations, while the IgG and antitoxin titers were suppressed by these formulations. CpG-ODN as an adjuvant could increase the serum IgG and antitoxin titers when co-administered with TT solution or co-encapsulated with TT in PLGA nanospheres, but failed to potentiate the IgA titers in nasal lavages. No hemolysis was occurred on incubation of PLGA nanospheres and human (RBCs). Also after nasal administration of plain nanospheres to human volunteers, no local irritation was seen. Intranasal administration of nanospheres encapsulated with vaccines showed to be an effective way for inducing mucosal sIgA immune responses, and CpG-ODN could increase the systemic immune responses.

Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. In order to increase the drug dissolution, its solid dispersions were prepared by the cogrinding technique using an insoluble but highly hydrophilic crospovidone and soluble hydroxypropylmethylcellulose (HPMC) as the carriers. The ratios of drug to carrier were 1:1, 1:5 and 1:10. Comparison of the dissolution of the drug from its cogrounds with that of the unground drug, its ground form and the corresponding physical mixtures revealed considerable differences. The percentage of drug dissolved during the first 30 min, (%D30), for the ground and coground drug was 75-95, whereas the %D30 for unground drug and its physical mixtures ranged from 41-62. FT-IR spectra indicated no intraction between the drug and the carriers in the cogrounds. But reduced crystallinity of the drug in the ground and cogrounds was evident in the x-ray diffraction patterns. The decreased crystallinity together with a reduced particle size, enhanced deaggregation and increased wettability of the drug. This could be accounted for the increased dissolution from the cogrounds. From the dissolution point of view, the physical mixtures of HPMC were inferior to the cogrounds, but were slightly superior to the physical mixtures of crospovidone due to the solubilization effect of HPMC.

Shampoos are products which remove surface grease and dirt from the hair shaft and scalp. The cleansing or detergent action of a shampoo is a primary function. However, the foaming characteristic of a shampoo has an important role in its acceptability. Often alkanolamides are used for the formation of a stable foam; but because of producing nitrosamines, they are potentially carcinogenic compounds. Hence, the main goal of this study was the elimination of these materials from shampoo formulations. Acanthophyllum squarrosum is one of the 23 species of the genus Acanthophyllum endemic in Iran. Due to the presence of saponin in its root, chubak, has been used traditionally as a detergent. In this study, total saponins of Acanthophyllum squarrosum roots were extracted, using several solvents. A clear liquid shampoo base was formulated using Texapon as surfactant, sodium chloride as thickener, glycerin as viscosity modifier, methyl paraben as preservative and EDTA as sequestring agent. Then, a fixed amount of Texapon was substituted by 1, 2.5 and 5 percent of total herbal saponins. Foaming ability of the shampoos prepared was evaluated by the Ross-Miles method and the cleansing power by Thompson test. The best result was found with the formula containing 20% Texapon and 5% total herbal saponins. Therefore, this formulation was selected as the best formula and evaluated for other characteristics. In addition to possessing the properties of a liquid shampoo, the unique characteristics of the formula containing 5% total herbal saponins was that it produced a stable foam without the use of foam stabilizers. Evaluation of the cleansing power by Thompson test showed that the final formula is a shampoo for normal hair, with very good cleansing ability. Rheological studies showed that the final formula had a pseudoplastic behavior. Organoleptic and physicochemical characteristics of the final formula were all found to be acceptable.

The intake of antioxidants intake has been reported to be inversely associated with the incidence of coronary artery disease. To clarify the possible role of lipophilic antioxidants in prevention of atherosclerosis, we investigated the effects of lycopene on the susceptibility of low-density lipoprotein (LDL) to oxidative modification. In this study, “lycopene” was added to plasma and incubated for 3 h at 37°C. Then, the LDL fraction was separated by ultracentrifugation. The oxidizability of LDL was estimated by measuring conjugated dienes (CD), lipid peroxides and thiobarbituric acid-reactive substances (TBARS) after addition of cupric sulfate solution.We showed that lycopene significantly (P<0.01 by ANOVA) and dose-dependently prolonged the lag time before the initiation of oxidation reaction. Also, it suppressed the formation of lipid peroxides and TBARS more markedly than the control. LDL exposed to lycopene in vitro reduced oxidizability. These findings raise the possibility that lycopene has a role in ameliorating atherosclerosis.

Aflatoxins are a group of fungal toxic metabolites, which are contaminated certain food commodities. ELISA is one of the sensitive methods for detection of aflatoxins. Preparation and stabilizing of a proper conjugated tracer for detection of aflatoxins is probably the main step for designing an ELISA method. In current study, different stabilizers were applied to stabilize a newly prepared conjugated molecule, Horseradish peroxidase-Bovine serum albumin- Aflatoxin B1 (HRP-BSA-AFB1). Stabilizing effects of six different stabilizers were compared during 10 months verification at room temperature and 6 weeks verification at 37°C. Based on the results, it was concluded that trehalose-containing stabilizers especially those contain casein in their compositions show the best stabilizing effects on HRP-BSA-AFB1 conjugated tracer.

The mechanisms of drug dependence and rewarding properties of opiates are not exactly known and several neurotransmitters seem to be involved. It is possible that the rennin-angiotensin system could interact with the opioid system, since it has been shown that angiotensin II(Ang) and ACE inhibitors have analgesic, anticonvulsant and antidepression effects and in some cases they could antagonize the effect of morphine. In the present study, the effect of Ang II and captopril on withdrawal signs was evaluated.Male wistar rats were anesthetized and i.c.v cannula implanted and allowed to recover from surgery. Morphine was injected (i.p, 3 times a day) for 4 days to induce morphine dependence. The animals were divided into 3 groups and received saline, captopril, Ang II, and i.c.v, before naloxone injection. Naloxone precipitated morphine withdrawal signs, compared to the morphine dependent rats in saline, captopril and Ang II groups. Results showed that in the captopril group, some of the withdrawal signs were significantly lower than the saline group (p<0.05 and p<0.01). In the Ang II group, some of the withdrawal signs were greater than the saline group (p<0.01 and p<0.001). Considering the fact that captopril can reduce endogenous opioid degradation, it could probably reduce the morphine withdrawal signs in this way. On the other hand, captopril and Ang II can interact with dopamine, serotonin, substance p, acetylcholine or nitric oxide in different brain regions and alter morphine withdrawal signs.

Rosa damascena has been found to act on central nervous system including the brain. Several studies confirm that R. damascena inhibits the activity of the hypothalamus and pituitary systems in rat and can suppress the central nervous system. In traditional medicine hypnotic effect of Rose is also suggested. In this study, the hypnotic effect of the ethanol crude extract of R. damascena and its fractions was investigated in mice. Hypnotic method was based on prolongation pentobarbital induced sleeping time by the extract and fractions (with water, ethyl acetate and n-butanol). Two doses of extract and fractions (250 and 500 mg/kg) was injected intraperitoneal in comparison with diazepam (3 mg/kg) as the positive control and saline (10 ml/kg) as the negative control. Thirty minutes after injection of extract and fractions, pentobarbital (30 mg/kg) was injected and the increase in the sleeping time due to the extract and fractions was recorded. The results showed that the ethanol extract and fractions of R. damascena at 250 and 500 mg/kg doses prolonged the pentobarbital induced sleeping time in mice (P<0.05 to P<0.001). Among all fractions, aqueous fraction has the least, and the ethyl acetate fraction at 500 mg/kg dosage has the best hypnotic effect. In conclusion, the results of this study showed hypnotic effect of R. damascena which was more potent in ethyl acetate fraction.

Dementia is one of the age related mental problems and a characteristic symptom of various neurodegenerative disorders including Alzheimer’s disease. Desmodium gangeticum DC. (Leguminosae) is widely used in Ayurveda for treating various neurological disorders. In the present study, the effectiveness of aqueous extract of D. gangeticum in attenuating scopolamine-induced amnesia in mice was investigated. Passive avoidance paradigm was used to assess long-term memory. In order to delineate the possible mechanism through which D. gangeticum elicits the anti-amnesic effects, we studied its influence on central cholinergic activity by estimating the acetylcholine content of the whole brain and acetylcholinesterase activity at different regions of the mouse brain, viz., cerebral cortex, midbrain, medulla oblongata and cerebellum. Pretreatment with D. gangeticum (100 mg/kg and 200 mg/kg, p.o.) for seven successive days, reversed scopolamine induced amnesia in mice. D. gangeticum increased mice brain acetylcholine content and decreased acetyl cholinesterase activity in a similar manner to the standard cerebro-protective drug piracetam. Hence, aqueous extract of D. gangeticum can be used to delay the onset and reduce the severity of the symptoms of dementia and Alzheimer’s disease.

The current treatment of choice for cutaneous leishmaniasis is either parenteral or intralesional antimonial compounds. Each of these treatments has its own downfalls which include toxic side effects with the parentral injection and pain at the site of injection with the intralesional injection. In recent years, there has been more focus on Paromomycin as an alternative drug; however, current data arose many controversies. In this study, the efficacy of different therapeutic regimens including topical paromomycin 20%, topical gentamycin 0.5%, intralesional glucantime injections, topical paromomycin 20% combine with gentamycin 0.5%, and placebo were compared. The results showed that the topical application of paromomycin had better response, less recurrence. In conclusion, topical paromomycin 20% can be an appropriate substitute for intralesional injection of glucantime, but more studies are needed to support its efficacy in human cutaneous leishmaniasis.

Re-investigation of the methylene chloride extract of the roots of Ferula sinaica gave ferusinol, a new sesquiterpene coumarin with a rare carbon skeleton, and samarcandin diastereomer. The structures elucidation were determined by MS, 1H- 13C-1D and 2D NMR spectral data.