Iranian Journal of Pharmaceutical Sciences

The present study deals with the formulation and evaluation of chitosan nanoparticles containing donepezil hydrochloride for the targeted delivery to the brain. Nanoparticles were prepared by ionic gelation method using sodium tripolyphosphate (TPP) as a cross linking agent followed by sonication. Nanoparticles were obtained in the average size ranging from 116.8 to 227.5 nm. Particle morphology
was determined by scanning electron microscopy (SEM). The SEM image showed that each particle unit exhibited a nanostructure. Encapsulation efficiency of nanoparticles ranged between 46.66% and 70.41%. The prepared particles showed good drug-loading capacity. The in vitro release studies showed that after the initial burst, all of the drug-loaded batches provided a continuous and slow release of the
drug. Drug released profile was found to be a non-Fickian analomous diffusion, and the drug release was followed by first order kinetics. The drug loaded batches showed a good stability when stored at room temperature for 60 days. FT-IR studies indicated that there was no chemical interaction between the drug and polymer. The present study revealed that ionic gelation technique followed by sonication can be
used as an effective tool for preparation of donepezil nanoparticles, which may significantly improve its ability to cross BBB and enter CNS.

The purpose of this review article is to characterize all of the parameters regarding the types, polymers used, and release kinetics of matrix tablets. Matrix system was the earliest oral extended release platform for medicinal use. Matrix tablets are most commonly used methods to modulate the release profile of drugs. They are much desirable and preferred for such therapy because they offer better patient compliance, maintain uniform drug levels, reduce dose and side effects, and increase safety margin for high potency drugs. Hydrophilic polymer matrix systems are widely used for designing oral controlled drug delivery dosage forms because of their flexibility to provide a desirable drug release profile, cost effectiveness, and broad regulatory acceptance. However, the use of hydrophilic matrix alone for extending drug release for highly water soluble drugs is restricted due to rapid diffusion of the dissolved drug through the hydrophilic gel network. For such drugs it becomes essential to include hydrophobic polymers in the matrix system. This leads to the conclusion that matrix tablets seem to be most promising when developing an oral controlled release formulation.

The purpose of this study was to investigate the effect of additives, poly(ethylene glycol) (PEG) 1450, poloxamer 407, polyvinyl alcohol (PVA) and sodium chloride in order to improve physico-chemical characteristics, encapsulation efficiency and in vitro release of bovine serum albumin, form poly(D,L-lactic-co-glycolic acid) (PLGA) microparticles prepared by the w/o/w solvent evaporation method. The
addition of PEG 1450 and 0.05 M NaCl changed the surface characteristics of microparticles and also affected the encapsulation efficiency and burst release of protein. The effect of surfactants: polyvinyl alcohol and poloxamer 407 used in the outer water phase was investigated. The surfactant/PLGA mass ratio played an important role in the preparation procedure of the particles. This ratio was found to be approximately 0.5 for PVA and 5 for poloxamer 407 in order to achieve microparticles with narrow size distribution (<70 μm) and good encapsulation efficiency (>70%).

Punica granatum is used as a medicinal plant, and its fruit concentrate has been used for the prevention and treatment of liver diseases in Iran. The effects of different concentrations of the hydroalcoholic, ethyl acetate and n-hexane extracts of the Punica granatum (fruit juice and seed) were investigated against CCl4-induced cytotoxicity in HepG2 cells. Concentrations (1-10000 μg/ml) of the extracts were added to the cells, 1 h before the addition of 100 mM of CCl4. After 24 h, the cells were evaluated for toxicity, TBARs level and GSH content. The hydroalcoholic extracts of fruit juice and seeds with concentrations of 100 to 1000 μg/ml protected the cells against CCl4 induced cytotoxicity, but the ethyl acetate extract of fruit juice with higher concentration (1000 μg/ml) protected the cells against CCl4 cytotoxicity and the n-hexane extracts were less effective. The ethyl acetate and n-hexane extracts of seeds with different concentrations did not have any significant protective effect. The Punica granatum extracts themselves were not toxic towards cells with concentrations up to 1 mg/ml. Therefore, the results of the present study are somehow consistent with traditional beliefs about hepatoprotective effects of Punica granatum.

Medication errors (MEs) are the most common error in ICUs. In fact, 78% of all serious errors in ICUs are due to MEs. Therefore, detecting MEs has vital significance. The goal of this study was to investigate the frequency, type and consequences of different types of errors including prescribing, transcribing and administration errors in an ICU of a large teaching hospital. Disguised direct observation method was used to detect errors. A pharmacy student observed 307 doses in 46 days of 6 h shifts. Observation data were entered in a form designed specifically for this purpose. Two hundred and fourteen MEs were identified in 307 doses. This is equivalent to 69.7% of total error. The error breakdown is as follows: administration errors 43.1%, preparation errors 24.1% and transcription errors 2.5%. Administration techniques and monitoring were determined to be the most common errors of MEs. Nearly, 89.4% of errors did not result in imminent danger to the patients. In the ICU under this study, the most common MEs were administration and prescription errors. To improve the quality of care in the ICU and reduce MEs, efforts should be directed to correct the wrong administration technique and inappropriate monitoring. The use of pharmacy department in drug preparation instead of drug preparation by nurses, using protocols for IV infusions, providing equipment and trained personnel for therapeutic drug monitoring and measuring medications level may help reduce suboptimal drug prescription and administration.

In the present study, aqueous solutions of some copper-complexing ligands were screened for their cytotoxicity using brine shrimp lethality test. Among the ligands tested, diacetyl-bis(N4- methylthiosemicarbazones) (ATSM) proved to be the most safe and non-toxic compound (2% lethality at 10 ppm), while pyruvaldehyde Bis(N4-methyl)thiosemicarbazone (PTSM) was shown to possess low toxicity (7% lethality at 10 ppm) and glyoxal-bis-thiosemicarbazone (GTS) proved to be a toxic compound even at 1 ppm (20% lethality). An interesting structure-toxicity relationship was observed for the ligands based on their water solubility leading to more toxicity which can be related to polysaccharide crustae of the shrimps. Considering the 1-10 ppm to be the maximum possible concentration of the ligands in the final
pharmaceutical samples, the safety of these ligands are ATSM>PTSM>GTS.

Plants of Asteraceae are used in traditional medicine and phytotherapy. The two main caffeic acid derivatives, chicoric and caftaric acid which are found in many genus of Asteraceae including Echinacea exhibit important biological activities. The level of these acids in E. purpurea is affected by many factors such as growing situations, extraction methods, storage conditions and plant age. In this investigation,
chicoric acid and caftaric acid content in aerial parts and roots of E. purpurea harvested in spring and summer from 1-, 2- and 3-years old plants cultivated in Iran were determined by using HPLC method. The results revealed that maximum level of chicoric acid achieved in aerial parts of 1- and 2-years old plants beside 2-years old roots collected in spring. Aerial parts of 1- and 2-years old plants harvested in
spring had maximum content of caftaric acid as well. It is concluded that total parts of 2-years old E. purpurea harvested in spring can be a good source of caffeic acid derivatives and used for preparation of the plant products.

A series of N-substituted-2,4-thiazolidinedione derivatives (TZDs) were prepared via N-alkylation of 2,4-TZD at position 3 using substituted benzyl halides. Synthesized N-substituted-2,4-TZD was then substituted at position 5 with substituted aromatic aldehyde according to Knoevenagel condensation method. Structures of the compounds were elucidated using various spectral techniques viz. IR, 1HNMR. The synthesized compounds were evaluated for their antimicrobial activity.