The search for new anticonvulsant agent with more selectivity and lower toxicity continues to be an area of rigorous investigation in medicinal chemistry. Epilepsy is a chronic disorder of brain whose treatment consists of controlling seizures with antiepileptic drugs that very often related with side-effects which in rare circumstances can be potentially life-threatening. Triazolam and Alprazolam are established drugs used in epilepsy which have triazole moiety. The potency and broad spectrum of the pharmacological response of triazole moiety as anticonvulsant agent have attracted the attention of medicinal chemists to explore this framework for its potential. The literature shows that different substitution on triazole ring exhibit potent antiepileptic activity with no or lesser neurotoxicity. The present review is a sincere attempt to compile the reported potent triazole derivatives with significant anticonvulsant action.

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Bu çalışmanın amacı, glipizidin biyoyararlanımı arttırmak ve geleneksel dozaj formunun oral yoldan sık sık verilmesini elimine etmek için nanoteknoloji bazlı oral formülasyonlarını geliştirmektir. Glipizide, biyolojik olarak kısa yarı ömrü ve sınırlı oral biyoyararlanımı olan antidiyabetik bir ilaçtır. Yeni palmitik asit-pluronik F127-palmitik asit (PA-F127) pentablok kopolimer bazlı uzun süreli salım yapan glipizid nanopartikülleri (GNs) in vitro ve in vivo çalışmalar için hazırlanmış ve taranmıştır. Gereç ve Yöntemler: GN'ler yeni PA-F127 pentablok kopolimer kullanılarak solvent buharlaştırma yöntemi ile hazırlanmıştır. Hazırlanan nanopartiküller, partikül büyüklüğü, polidispersite indeksi (PDI), zeta potansiyeli, yükleme etkinliği, yüzde verimi ve fourier transform kızılötesi spektroskopisi (FTIR) ve diferansiyel tarama kalorimetresi (DSC) analizi, X-ışını kırınımı kullanılarak etken madde ile eksipiyan geçimliliği, taramalı elektron mikroskobu, in vitro etken madde salım çalışmaları, stabilite çalışmaları ve in vivo farmakokinetik çalışmalar değerlendirildi. Bulgular: FTIR ve DSC analizlerinin sonuçları, etken madde-eksipiyan etkileşimlerinin olmadığını göstermiştir. Optimize edilmiş GN1'in, partikül büyüklüğü 242.60±4.20 nm, PDI 0.171±0.014 ve zeta potansiyeli-21.41±0.462 mV idi. Hazırlanan nanopartiküller küreseldi ve yarı amorf özellikler göstermiştir. İn vitro salım çalışmaları, ilk 8 saatte %34.43±4.8 etken madde salındığını ve 24 saat içinde 56.11±%4.12 glipizid salındığını göstermiştir. GN1'in 5±3°C'de 3 aya kadar stabil olduğu bulunmuştur. Farmakokinetik çalışmalar, oral yoldan verilen GN1'in, saf glipizide göre 2.35 kat C max , 1.6 kat t max , 3.3 kat eğri altındaki alan (AUC 0→∞) ve 1.2 kat ortalama kalış süresi ile daha üstün olduğunu göstermiştir (p<0.05). Sonuç: Yeni geliştirilen GN1'in biyoyararlanımı başarılı bir şekilde arttırılmıştır ve diyabet tedavisi için ticari dozaj formu ile sık sık oral uygulama sorunu aşılabilmiştir. Anahtar kelimeler: Glipizid, nanopartiküller, palmitik asit, pluronikler, biyoyararlanım Objectives: The aim of the present study was to develop nanotechnology-based oral formulations of glipizide to enhance the bioavailability and eliminate the frequent oral administration of the conventional dosage form. Glipizide is an antidiabetic drug with a short biological half-life and limited oral bioavailability. Novel palmitic acid-pluronic F127-palmitic acid (PA-F127) pentablock copolymer-based prolonged release glipizide nanoparticles (GNs) were prepared and screened for in vitro and in vivo studies. Materials and Methods: GNs were prepared using a novel PA-F127 pentablock copolymer by solvent evaporation technique. The prepared nanoparticles were evaluated for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, percentage yield, and drug excipient compatibility using fourier transform infrared spectroscopy (FTIR) and differential scanning calorimeter (DSC) analysis, X-ray diffraction, scanning electron microscopy, in vitro drug release studies, ...

Objective: The objective of this study was to prepare and evaluate metformin nanoparticles (MN) using stearic acid-coupled F127 (SAF127) copolymer and polyvinyl alcohol by emulsion solvent evaporation technique.Method: Metformin is the first-line drug for the treatment of type II diabetes mellitus belongs to Biopharmaceutical Classification System Class III. The prepared MN was characterized for particle size, polydispersity index (PDI), zeta potential, drug entrapment, percentage yield, in vitro drug release, and stability studies. The compatibility studies were performed by Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC). The crystallographic and surface properties were studied by X-ray diffractometry and scanning electron microscopy, respectively.Results: The mean particle diameter of prepared nanoparticles ranged from 207.8 to 977.64 nm, PDI value ranged from 0.146 to 0.694, and zeta potential ranged from −20.5 to −6.97 mV. The drug entrapment efficiency of these nanoparticles varies between 18.81 to 69.01 %. The drug to SAF127 copolymer (10/30 w/w) ratio (MN3) showed optimum results. The MN3 had spherical morphology with semi-amorphous nature. The results of FTIR and DSC analysis showed that there was no significant interaction between drug and excipients. The prepared polymeric nanoparticles were stable at 5±3°C up to 3 months. In vitro release of drug from MN3 was 20.52% in the first 1 h and remaining drug was released up to 30 h.Conclusion: The results of this study confirmed the sustained drug release profile of metformin loaded SAF127 copolymer nanoparticles. These nanoparticles can be best stored up to 3 months.

In the modern system of drug delivery, even after several efforts by the scientists, the chief key issue remains the efficient and effective amount of drug delivery at particular site. Due to the low residence time of API's at the required site, leads to the poor bioavailability of drugs in the conventional drug delivery systems. At present nanotechnology is the emerging field for delivery of drugs at size of nano-scale and very effective in sustained and targeted delivery of medicines i.e. polyplexes (DNA/polycation complexes), block copolymer micelles and nano-gels etc. In the human trials, polymeric micelles have been found to be very convincing method for delivery of anticancer drugs. Selection of suitable method of preparation remain an important aspect as particulate systems like nanoparticles have been used as a physical approach to alter and improve the pharmacokinetic and pharmacodynamics properties of various types of drug molecules. Several methods to prepare polymeric nanoparticles have been developed and these techniques are classified according to whether the particle formation involves a polymerization reaction or nanoparticles form directly from a macromolecule or preformed polymer.