scholarly journals Oral Bioavailability and Lymphatic Transport of Pueraria Flavone-Loaded Self-Emulsifying Drug-Delivery Systems Containing Sodium Taurocholate in Rats

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 147 ◽  
Author(s):  
Jin Qiao ◽  
Danyang Ji ◽  
Shilin Sun ◽  
Guangyuan Zhang ◽  
Xin Liu ◽  
...  

We developed self-microemulsifying drug-delivery systems (SMEDDS), including bile salts, to improve the oral bioavailability of pueraria flavones (PFs). The physical properties of the SMEDDS using Cremophor RH 40, and bile salts as mixed surfactants at weight ratios of 10:0–0:10 were determined. The particle sizes of PFs-SMEDDSNR containing sodium taurocholate (NaTC) and Cremophor RH 40, and PFs-SMEDDSR containing Cremophor RH 40 were measured upon dilution with deionized water and other aqueous media. Dilution volume presented no remarkable effects on particle size, whereas dilution media slightly influenced particle size. PFs-SMEDDSNR and PFs-SMEDDSR provided similar release rates in pH-1.2 hydrochloride solution. However, the release rate of PFs-SMEDDSNR was faster than that of PFs-SMEDDSR in pH-6.8 phosphate buffer containing 20 mM NaTC and 500 U/mL porcine pancreas lipase. The pharmacokinetics and bioavailability were measured in rats. The oral bioavailability of PFs-SMEDDSNR was 2.57- and 2.28-fold that of a suspension of PFs (PFs-suspension) before and after the blockade of the lymphatic transport route by cycloheximide, respectively. These results suggested PFs-SMEDDSNR could significantly improve the oral relative absorption of PFs via the lymphatic uptake pathway. SMEDDS containing NaTC may provide an effective approach for enhancing the oral bioavailability of PFs.

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Samatha Akula ◽  
Aravind Kumar Gurram ◽  
Srinivas Reddy Devireddy

Ease of administration and painless approach made oral route the most preferred. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of dissolution rate limited absorption. Failure to attain intended therapeutic effect of the poor water soluble drugs by this route led to development of novel drug delivery systems which will fulfill therapeutic needs with minimum dose. Although many formulation approaches like solid dispersions, complexation, pH modification, and cocrystals exist, lipid based delivery systems finding increased appliance with the apparent increase in absorption of drug. Among lipid based formulations, self-microemulsifying formulations (droplet size < 100 nm) are evident to improve the oral bioavailability of hydrophobic drugs primarily due to their efficiency in facilitating solubilization and in presenting the hydrophobic drug in solubilized form whereby dissolution process can be circumvented. Various components that are used to formulate these dosage forms like surfactants and lipids contribute to the overall improvement in oral bioavailability via promoting the lymphatic transport; thereby hepatic first pass metabolism can be surmounted. The present paper gives exhaustive information on the formulation design and characterization of SMEDDS along with the probable mechanisms by which the bioavailability can be improved with SMEDDS.


2012 ◽  
Vol 39 (9) ◽  
pp. 1431-1438 ◽  
Author(s):  
Gun Gook Kim ◽  
Bijay K. Poudel ◽  
Nirmal Marasini ◽  
Dong Won Lee ◽  
Tran Tuan Hiep ◽  
...  

2019 ◽  
Vol 52 ◽  
pp. 597-606 ◽  
Author(s):  
Na Man ◽  
Qilong Wang ◽  
Huihua Li ◽  
Michael Adu-Frimpong ◽  
Congyong Sun ◽  
...  

2016 ◽  
Vol 7 (4) ◽  
pp. 887-898 ◽  
Author(s):  
Stefano Stefani ◽  
Indah N. Kurniasih ◽  
Sunil K. Sharma ◽  
Christoph Böttcher ◽  
Paul Servin ◽  
...  

A set of biodegradable nanocarriers characterized by a hyperbranched polyester core and an amphiphilic branched shell was developed and employed to efficiently solubilize hydrophobic drugs in aqueous media.


2010 ◽  
Vol 36 (11) ◽  
pp. 1356-1363 ◽  
Author(s):  
Bing Shao ◽  
Jingling Tang ◽  
Hongyu Ji ◽  
Hongmei Liu ◽  
Yan Liu ◽  
...  

2009 ◽  
Vol 374 (1-2) ◽  
pp. 66-72 ◽  
Author(s):  
Prabagar Balakrishnan ◽  
Beom-Jin Lee ◽  
Dong Hoon Oh ◽  
Jong Oh Kim ◽  
Young-Im Lee ◽  
...  

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