Thiolated chitosan nanoparticles for augmented oral bioavailability of gemcitabine: Preparation, optimization, in vitro and in vivo study

Author(s):  
Amandeep Kaur ◽  
Parveen Kumar ◽  
Loveneet Kaur ◽  
Rohit Sharma ◽  
Preeti Kush
2015 ◽  
Vol 51 (2) ◽  
pp. 467-477 ◽  
Author(s):  
Abdul Baquee Ahmed ◽  
Ranjit Konwar ◽  
Rupa Sengupta

<p>In this study, we prepared atorvastatin calcium (AVST) loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, <italic>in vitro</italic> release and surface morphology by scanning electron microscopy (SEM). In addition, the pharmacokinetics of AVST from the optimized formulation (FT5) was compared with marketed immediate release formulation (Atorva<sup>(r))</sup> in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI) value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. <italic>In vitro</italic> release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC) of the optimized formulation as compared to marketed formulation (Atorva<sup>(r))</sup>. Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model.</p>


2011 ◽  
Vol 59 (2) ◽  
pp. 272-278 ◽  
Author(s):  
Ramesh Chand Nagarwal ◽  
Paras Nath Singh ◽  
Shri Kant ◽  
Pralay Maiti ◽  
Jayanta Kumar Pandit

RSC Advances ◽  
2015 ◽  
Vol 5 (99) ◽  
pp. 81728-81738 ◽  
Author(s):  
Rohan D. Deshpande ◽  
Gowda D. V. ◽  
Naga Sravan Kumar Varma Vegesna ◽  
Rudra Vaghela ◽  
Kulkarni P. K.

In the present study, efforts were made to optimize the process parameters of LAS technique for developing GLB NPs, in order to enhance the aqueous solubility as well as oral bioavailability.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Shahrooz Saremi ◽  
Rassoul Dinarvand ◽  
Abbas Kebriaeezadeh ◽  
Seyed Nasser Ostad ◽  
Fatemeh Atyabi

The aim of this study was to evaluate a nanoparticulate system with mucoadhesion properties composed of a core of polymethyl methacrylate surrounded by a shell of thiolated chitosan (Ch-GSH-pMMA) for enhancing oral bioavailability of docetaxel (DTX), an anticancer drug. DTX-loaded nanoparticles were prepared by emulsion polymerization method using cerium ammonium nitrate as an initiator. Physicochemical properties of the nanoparticles such as particle size, size distribution, morphology, drug loading, and entrapment efficiency were characterized. The pharmacokinetic study was carried out in vivo using wistar rats. The half-life of DTX-loaded NPs was about 9 times longer than oral DTX used as positive control. The oral bioavailability of DTX was increased to 68.9% for DTX-loaded nanoparticles compared to 6.5% for positive control. The nanoparticles showed stronger effect on the reduction of the transepithelial electrical resistance (TEER) of Caco-2 cell monolayer by opening the tight junctions. According to apparent permeability coefficient (Papp) results, the DTX-loaded NPs showed more specific permeation across the Caco-2 cell monolayer in comparison to the DTX. In conclusion, the nanoparticles prepared in this study showed promising results for the development of an oral drug delivery system for anticancer drugs.


2008 ◽  
Vol 349 (1-2) ◽  
pp. 226-233 ◽  
Author(s):  
Fu Chen ◽  
Zhi-Rong Zhang ◽  
Fang Yuan ◽  
Xuan Qin ◽  
Minting Wang ◽  
...  

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