Medicinal Chemistry

Aim: Evaluation of the effect of substitution therapy on the birth weight of the newborn, its postpartum adaptation and course of the neonatal abstinence syndrome.
Patients and methods: We studied heroin-addicted women and women undergoing methadone and buprenorphine substitution. During the 3 years we concentrated on 47 heroin-addicted women and 60 women under substitution for prenatal screening, labour and delivery.
Results: Birth weight of newborns was lowest in the group of heroin-addicted women as compared to the group receiving substitution with buprenorphine p < 0.01 and to the group of methadone-substituted patients p < 0.05. The highest number of changes in the placenta was exhibited by heroin users, both when compared to methadone users (p < 0.01) and buprenorphine users (p < 0.001). The highest statistically significant number of newborns with IUGR symptoms were born to heroin-addicted women. The lowest Apgar score was recorded in all three evaluations in the group of buprenorphine users and the highest in methadone-substituted women.
Conclusions: Substitution therapy provides pregnant women with the possibility of social stabilization and
adequate prenatal care. With regard to the fact that methadone substitution protracts the newborn´s abstinence syndrome, attention has been recently focused on substitution with buprenorphine that seems to be from this viewpoint a more considerate option.

Purpose: This article describes the preparation and characterization of folate conjugated nanoparticles using poly(lactide-co-glycolide)-poly(ethylene glycol)-folate (PLGA-PEG-FOL) polymer for targeted delivery of anticancer agents. Methods: PLGA-PEG-FOL was synthesized by coupling di-block copolymer (PLGA-PEG-NH2) with folic acid. PLGA-PEG-FOL polymer was characterized by 1H NMR, GPC and FTIR. PLGA-PEG-FOL polymer was employed in the preparation of doxorubicin (DOX) loaded nanoparticles by double emulsion solvent evaporation (DESE), single emulsion solvent evaporation (SESE) and dialysis methods. Nanoparticles were characterized for size, morphology, entrapment efficiency, in vitro release and folate content. The presence of folate on nanoparticle surface was also confirmed using transmission electron microscopy. Qualitative uptake and cell viability studies were carried out in FOL receptor-positive ovarian cancer cells (SKOV3).
Results: DESE and SESE methods resulted in folate conjugated nanoparticles with an average size of 200 nm and entrapment efficiencies of 24.5 and 51.9% respectively. However, dialysis method resulted in microparticles with an average size of 2.5 μm. Folate conjugated nanoparticles exhibited higher uptake and cytotoxicity in SKOV3 cells in comparison with the pure DOX and unmodified nanoparticles.
Conclusion: PLGA-PEG-FOL can be utilized in the preparation of surface modified nanoparticles for targeted
delivery of anticancer agents to FOL-receptor-positive cancer cells.

The aim of the present investigation was to prepare and evaluate gastroretentive floating microspheres of Verapamil hydrochloride that would retain the drug in stomach and continuously release the drug in controlled manner up to a predetermined time. Floating microspheres were prepared by emulsion solvent evaporation technique. In the present investigation three polymers were used in various concentrations; Methocel K4M, Methocel K15M and Methocel K100M. In vitro performance was evaluated by the usual pharmacopoeial and other tests such as particle size analysis, drug entrapment efficiency, flow properties, in vitro floatability studies, in vivo floatability studies in dog, in vitro drug release studies, stability studies etc. Results showed that the mixing ratio of components in the organic phase affected the size, size distribution, yield, drug content, floating time and drug release of microspheres. In most cases good in vitro floating behavior was observed and a broad variety of drug release pattern could be achieved by variation of the drug, polymer and solvent ratio.

Clove has a large number of therapeutic properties and its tea has been used by the general population as antiinflammatory, antihyperglycemic, antimutagenic, bactericidal, and nematicidal, among others. Thus, the aim of this study was to assess the effect of clove on biochemical parameters of rats subjected to ethanol consumption and abstinence. The animals were subjected to ethanol intake before and after treatment with clove tea, according to their groups, as follows: GW received water (control); GE received 3% ethanol alone; GC received clove alone; GCE received clove for 7 consecutive days followed by 3% ethanol for 16 consecutive days; GEC received 3% ethanol for 16 consecutive days followed by clove for 7 consecutive days. Administration of clove tea alone or ethanol alone did not change serum parameters such as glucose, triglycerides, total cholesterol, total protein and albumin, and it did not alter weight gain although there was a significant difference in mean food consumption, which suggests that under such conditions clove tea or ethanol does not interfere with these parameters. On the other hand, administration of clove tea before or after ethanol administration led to significant changes in several parameters such as glucose, triglycerides, cholesterol, total protein and albumin. The obtained results thus suggest that prolonged ethanol intake should be avoided when clove tea is consumed daily.