Polimerik nanopartiküller kanser tedavisinde avantajlı ve gelecek vaad eden yeni ilaç salım sistemidir. Etopozid, çeşitli malignitelerin tedavisinde kullanılan bir antikanser ajanıdır. Bu çalışmanın amacı, etopozit içeren yeni polimerik nanopartiküllerin hazırlanması ve değerlendirilmesidir. Gereç ve Yöntemler: Eudragit EPO ve Pluronic F-68'in nanopartikül süspansiyonunun karakterizasyonu üzerindeki etkisini incelemek için 3 2 tam faktöriyel tasarım kullanılmıştır. Polimerik nanopartiküller nano presipitasyon tekniği ile hazırlanmıştır. Hazırlanan nanopartiküller, yüzde verim, fourier dönüşümü kızılötesi (FTIR) spektroskopisi ve diferansiyel taramalı kalorimetrik (DSC) analizi kullanılarak ilaç polimer uyumluluğu, etkin madde içeriği, yükleme kapasitesi, zeta potansiyeli, partikül boyutu, taramalı elektron mikroskobu, X-ışını difraksiyon, in vitro etkin madde salım

Objectives: Polymeric nanoparticles is a promising novel drug delivery system and have advantageous in cancer therapy. Etoposide is an anticancer agent that is used in the treatment of a variety of malignancies. The present study was aimed to prepare and evaluate the Novel polymeric nanoparticles containing etoposide. Materials and Methods: 3 2 full factorial design was used to study the effect of Eudragit EPO and Pluronic F-68 on characterization of nanoparticles suspension. The polymeric nanoparticles was prepared by nano-precipitation technique. The prepared nanoparticles was evaluated by percentage yield, drug polymer compatibility using FTIR and DSC analysis, drug content, entrapment efficiency, zeta potential, particle size, SEM, XRD, In-vitro drug release studies, kinetic modeling, stability studies and in-vivo animal study. Response surface plots were studied which was generated using PCP dissolution software. Results: Scanning electron microscopic studies confirmed their porous structure with number of nanochannels. The FTIR spectra showed stable character of etoposide in mixture of polymers and revealed the absence of drug polymer interactions. DSC study revealed that drug was involved in complexation with nanoparticles. The average particle size of etoposide nanoparticles was found to be in the range of 114.4 nm to 136.7 nm. The results of zeta potential values were attained to u n c o r r e c t e d p r o o f ensure a good stability of nanosuspensions. In-vitro release of drug from nanoparticles follows peppas and showed controlled release behavior for a period of 24 h. The optimized nanoparticles were subjected to stability studies at 4ºC in refrigerator and found most suitable temperature for storage of Etoposide nanoparticles. The average targeting efficiency of drug loaded nanoparticles was found to be 41.88 ±0.030% of the injected dose in liver, 25.66±0.320% in spleen 13.82±0.090% in lungs, 4.52±0.300% in kidney and 4.18±0.490% in brain. Conclusions: The study concluded that etoposide nanoparticles could be effective in sustained release and the drug loaded nanoparticles.

The aim of present investigation was to develop an optimized buccoadhesive film of metoprolol tartrate, a BCS class I drug, to provide unidirectional sustained drug delivery to the buccal mucosa that has potential to enhance the bioavailability. The films were prepared using HPMC K4M as film former, carbopol 934 P as buccoadhesive polymer and dimethyl sulfoxide as penetration enhancer, by solvent casting technique. The films were characterized for various pharmacotechnical parameters and 2 3 full factorial design was employed to study the effect of independent variables. The design was validated by extra design checkpoint formulation (BF9). The response of design was employed to study the effect of independent variables. The responses of design were analyzed using Design Expert 8.0.7.1 and the analytical tools of software were used to draw pareto charts. On the basis of software analysis, formulation BF4 with desirability factor of 0.698 was selected as optimized formulation and was evaluated for independent parameters. Optimized formulation showed 12.05 hr, ex-vivo residence time, and good permeation (42.68%) through goat buccal mucosa and 82.19% drug release after 8 th hour. The release kinetics of optimized formulation best fitted the higuchi model. Histopathological studies revealed no buccal mucosal damage. Hence BF4 formulation can be concluded as promising drug delivery system to enhance the permeability limited absorption of metoprolol tartrate.

In the present work, orodissolving tablets of Efavirenz were prepared by direct compression method with a view to enhance patient compliance. A 23 full factorial design was applied to investigate the combined effect of three formulation variables. Amount of crospovidone, croscarmellose sodium and sodium starch glycolate were used as superdisintegrant material along with direct compressible mannitol to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time, drug content and in-vitro dissolution studies. Based on wetting time, disintegration time, the formulation containing crospovidone (5% w/v), carscarmellose sodium (5% w/v) and sodium starch glycolate (8% w/v) was found to be promising and tested for in-vitro drug release pattern (in 0.1 N HCl), short term stability and drug-superdisintegrants interaction. Surface response plots are presented to graphically represent the effect of independent variables (conc. of superdisintegrants) on the in-vitro dissolution time. The validity of the generated mathematical model was tested by preparing extra-design check point formulation. The formulation showed nearly faster drug release compared to the conventional commercial tablet formulation. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, hardness, disintegration time, drug content and in-vitro drug release.