Effects ofN-trimethyl chitosan chloride as an absorption enhancer on properties of insulin liquid suppository in vitro and in vivo

2005 ◽  
Vol 99 (3) ◽  
pp. 1140-1146 ◽  
Author(s):  
Wen He ◽  
Yumin Du ◽  
Wenbing Dai ◽  
Yan Wu ◽  
Mian Zhang
2018 ◽  
Vol 16 (1) ◽  
pp. 86-92 ◽  
Author(s):  
Sang Hoon Lee ◽  
Yeo-song Lee ◽  
Jae Geun Song ◽  
Hyo-Kyung Han

Background: Chrysin is a strong inhibitor of breast cancer resistance protein (BCRP) but it is practically insoluble in water. Effective solubilization of chrysin is critical for its pharmaceutical application as an absorption enhancer via inhibition of BCRP-mediated drug efflux. Objective: This study aimed to develop an effective oral formulation of chrysin to improve its in vivo effect as an absorption enhancer. Method: Solid dispersions (SDs) of chrysin were prepared with hydrophilic carriers having surface acting properties and a pH modulator. In vitro and in vivo characterizations were performed to select the optimal SDs of chrysin. Results: SDs with Brij&®L4 and aminoclay was most effective in increasing the solubility of chrysin by 13-53 fold at varying drug-carrier ratios. Furthermore, SDs significantly improved the dissolution rate and extent of drug release. SDs (chrysin: Brij&®L4: aminoclay=1:3:5) achieved approximately 60% and 83% drug release within 1 h and 8 h, respectively, in aqueous medium, while the dissolution of the untreated chrysin was less than 13%. XRD patterns indicated the amorphous state of chrysin in SDs. The SD formulation was effective in improving the bioavailability of topotecan, a BCRP substrate in rats. Following oral administration of topotecan with the SDs of chrysin, the Cmax and AUC of topotecan was enhanced by approximately 2.6- and 2-fold, respectively, while the untreated chrysin had no effect. Conclusion: The SD formulation of chrysin with Brij&®L4 and aminoclay appeared to be promising in improving the dissolution of chrysin and enhancing its in vivo effect as an absorption enhancer.


2006 ◽  
Vol 110 (2) ◽  
pp. 353-361 ◽  
Author(s):  
Bogdan I. Florea ◽  
Maya Thanou ◽  
Hans E. Junginger ◽  
Gerrit Borchard
Keyword(s):  

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

2010 ◽  
Vol 144 (1) ◽  
pp. 46-54 ◽  
Author(s):  
Xin Zhao ◽  
Lichen Yin ◽  
Jieying Ding ◽  
Cui Tang ◽  
Shaohua Gu ◽  
...  

RSC Advances ◽  
2015 ◽  
Vol 5 (127) ◽  
pp. 105149-105159 ◽  
Author(s):  
Maria Letizia Manca ◽  
José E. Peris ◽  
Virginia Melis ◽  
Donatella Valenti ◽  
Maria Cristina Cardia ◽  
...  

This work was aimed at deliver curcumin to lungs by its incorporation into innovative vesicles glycerosomes and polymer-glycerosomes, the latter obtained combining glycerosomes with two polymers: sodium hyaluronate and trimethyl chitosan.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 409 ◽  
Author(s):  
Ali M. Nasr ◽  
Mona K. Qushawy ◽  
Mahmoud M. Elkhoudary ◽  
Aya Y. Gawish ◽  
Sameh S. Elhady ◽  
...  

Drug absorption from the gastrointestinal tract (GIT) is one of the major problems affecting the bioavailability of orally absorbed drugs. This work aims to enhance Fexofenadine HCl oral bioavailability in vivo, the drug used for allergic rhinitis. In this study, novel spray-dried lactose-based enhanced in situ forming vesicles were prepared using different absorption enhancer by the slurry method. Full factorial design was used to obtain an optimized formulation, while central composite design was used to develop economic, environment-friendly analysis method of Fexofenadine HCl in plasma of rabbits. The optimized formulation containing Capryol 90 as absorption enhancer has a mean particle size 202.6 ± 3.9 nm and zeta potential −31.6 ± 0.9 mV. It achieved high entrapment efficiency of the drug 73.7 ± 1.7% and rapid Q3h release reaches 71.5 ± 2.7%. The design-optimized HPLC assay method in rabbit plasma could separate Fexofenadine HCl from endogenous plasma compounds in less than 3.7 min. The pharmacokinetic study and the pharmacological effect of the fexofenadine-loaded optimized formulation showed a significant increase in blood concentration and significantly higher activity against compound 48/80 induced systemic anaphylaxis-like reactions in mice. Therefore, enhanced in situ forming vesicles were effective nanocarriers for the entrapment and delivery of Fexofenadine HCl.


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