scholarly journals Formulation and Evaluation of Stavudine Loaded Polymethacrylic Acid Nanoparticles

2013 ◽  
Vol 2 (4) ◽  
pp. 133-140 ◽  
Author(s):  
T Mallamma ◽  
DR Bharathi ◽  
R Yogananda ◽  
G Lakshmi Radhika ◽  
T Vyjayanhimala

Nanoparticles represent a promising drug delivery system of controlled and targeted drug release. They are specially designed to release the drug in the vicinity of target tissue. The aim of this study was to prepare and evaluate polymethacrylic acid nanoparticles containing stavudine in different drug to polymer ratio by nanoprecipitation method to be 121 + 8 to 403 + 4 nm. The particle size of the nanoparticles was gradually increased with increase in the proportion of polymethacrylic acid polymer. The drug content of the nanoparticles was increasing on increasing polymer concentration up to a particular concentration. No appreciable difference was observed in the extent of degradation of product during 60 days in which, nanoparticles were stored at various temperatures. FT-IR studies indicated that there was no chemical interaction between drug and polymer and stability of drug. The in-vitro release behavior from all the drug loaded batches was found to be zero order and provided sustained release over a period of 24 h. The developed formulation overcome and alleviates the drawbacks and limitations of stavudine sustained release formulations and could possibility be advantageous in terms of increased bioavailability of stavudine. DOI: http://dx.doi.org/ International Journal of Pharmaceutical and Life Sciences Volume 2, Issue 4: October 2013; 133-140

Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 


2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.


2015 ◽  
Vol 13 (1) ◽  
pp. 75-81 ◽  
Author(s):  
KR Naga Priya ◽  
Sayani Bhattacharyya ◽  
P Ramesh Babu

The present work focuses on formulation of erodible ocular films of valacyclovir hydrochloride (VH) for the treatment of ocular herpes to enhance therapeutic effect through prolonging contact time with the corneal surface. Nine films were prepared by solvent casting method using different ratios of polymers HPMC E 15 LV and PVP. The FT-IR studies showed no interaction between drug and the polymers. Developed formulations were evaluated for tensile strength, % elongation at break, strain, folding endurance, uniformity of thickness, weight variation, % moisture absorption, surface pH, drug content, in vitro release, kinetics study, sterility test and eye irritancy test on Rabbit eye. On the basis of these evaluations it was found that with increase in hydrophilic polymer content the mechanical properties and release rate of the films were improved. The kinetic study revealed case II transport. The eye irritancy test showed that the films were free from ocular toxicity and irritancy. DOI: http://dx.doi.org/10.3329/dujps.v13i1.21866 Dhaka Univ. J. Pharm. Sci. 13(1): 75-81, 2014 (June)


2017 ◽  
Vol 1 (2) ◽  
pp. 01-04
Author(s):  
Saritha Garrepalli

Prepared nanoparticles were characterized in terms of particle size, scanning electron microscope (SEM), fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). In-vitro release studies were performed in phosphate buffer saline pH 7.4 at 37˚±0.5˚C for 1month. The mean particle size of obtained nanoparticles was 150-400 nm and was apparently spherical in shape, with smooth surface. DSC is done for the stability test for pure drug and sample. The thermogram of drug has not shifted for in the formulation compare to pure drug thermogram hence, the stability of formulation is not changed. FT-IR studies demonstrated that the drug was not changed in the formulation during the fabrication process.The encapsulation efficiency was about 48%. The Anastrozole-BSA nanoparticles exhibit a most interesting release profile with small initial burst followed by slower and controlled release.


Author(s):  
Shravan Kumar Y ◽  
Shireesha G ◽  
Harika S

The objective of the present work was to develop sustained release matrix tablets of Metoprolol tartrate using different polymers viz. Guar gum, Xanthan gum, Kondagogu gum and HPMC K100M. The release rates were modulated by combination of two different rates controlling material and triple mixture of two different rate controlling materials. After evaluation of physical properties of tablet, the in-vitro release study was performed in phosphate buffer pH 6.8 up to 12 hrs. Dissolution data was analyzed for release kinetics. It was observed that matrix tablets contained polymer Xanthan gum was successfully sustained the release of drug up to 12 hrs. Among all the formulations, F6 which contains 45 % of Xanthan gum, release of drug which follows zero order kinetics via, swelling, diffusion and the release profile of formulation F6 was compared with marketed product. The FTIR study revealed that there was no chemical interaction between drug and excipient.


INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (07) ◽  
pp. 31-38
Author(s):  
Gurudev Kruthi ◽  
◽  
B. V. Basavaraj ◽  
S. Bharath ◽  
R. Deveswaran ◽  
...  

The main aim of the present work was to formulate and evaluate sustained release multiparticulate gastroretentive delivery system of cinnarizine. The microspheres were prepared by solvent evaporation method by using Eudragit RS 100 as a polymer in varying ratios. The prepared microspheres were evaluated for drug – polymer compatibility studies, micromeritic properties, drug entrapment efficiency, in vitro buoyancy and drug release studies. The mean particle size increased with increase in polymer concentration, ranging between 60.33 μm to 144.88 μm. FT IR studies showed that the drug and polymer were compatible with each other. The entrapment efficiency decreased with increase in the polymer concentration with values of 50%, 33.3% and 25% respectively. The microspheres floated upto 9 h over the surface of the gastric buffer medium and the buoyancy percentage was found to be in the range of 64.3 – 76.2%. In vitro drug release studies showed that the prepared microspheres exhibited prolonged drug release upto 62.89% for more than 9 h. The mechanism of drug release was found to be a combination of both peppas and matrix kinetics. Thus the developed floating microspheres of cinnarizine may be used as sustained drug delivery system for increasing the therapeutic efficacy with an improved patient compliance.


2014 ◽  
Vol 1051 ◽  
pp. 21-28 ◽  
Author(s):  
Xiang Dong Mei ◽  
Yan Hui Liang ◽  
Tao Zhang ◽  
Jun Ning ◽  
Zhong Yue Wang

In the present study, an amphiphilic chitosan-polylactide (CS-PLA) graft copolymer was synthesized through grafting polylactide (PLA) onto water-soluble chitosan (CS), and the chemical structure of this newly developed copolymer was confirmed by FT-IR, 1H NMR and thermogravimetric analysis (TGA). Stable flusilazole-loaded nanoparticles (NS), with a size near 280.3 nm and a loading content (LC) of 29.0%, were prepared for the fungicide delivery using a nanoprecipitation method. Moreover, size, size distribution and the flusilazole LC as well as the in vitro release profile of flusilazole-loaded NS were investigated. In conclusion, the NS could provide a controlled release of flusilazole and enhance the penetration of flusilazole in the plant compared with classical flusilazole emulsifiable concentrate (EC) formulation due to their small particle size. Therefore, the CS-PLA NS could be used as fungicide carriers for the flusilazole delivery system.


Author(s):  
Shanmuganathan S. ◽  
Nigma S. ◽  
Anbarasan B. ◽  
Harika B.

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.


Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.


Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.


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