Enhanced Oral Absorption of Paclitaxel in a Novel Self-Microemulsifying Drug Delivery System with or Without Concomitant Use of P-Glycoprotein Inhibitors

AC1497 is an effective dual inhibitor of malate dehydrogenase 1 and 2 targeting cancer metabolism. However, its poor aqueous solubility results in low bioavailability, limiting its clinical development. This study was conducted to develop an effective self-nanoemulsifying drug delivery system (SNEDDS) of AC1497 to improve its oral absorption. Based on the solubility of AC1497 in various oils, surfactants, and cosurfactants, Capryol 90, Kolliphor RH40, and Transcutol HP were selected as the components of SNEDDS. After testing various weight ratios of Capryol 90 (20–30%), Kolliphor RH40 (35–70%), and Transcutol HP (10–35%), SNEDDS-F4 containing 20% Capryol 90, 45% Kolliphor RH40, and 35% Transcutol HP was identified as an optimal SNEDDS with a narrow size distribution (17.8 ± 0.36 nm) and high encapsulation efficiency (93.6 ± 2.28%). Drug release from SNEDDS-F4 was rapid, with approximately 80% of AC1497 release in 10 min while the dissolution of the drug powder was minimal (<2%). Furthermore, SNEDDS-F4 significantly improved the oral absorption of AC1497 in rats. The maximum plasma concentration and area under the plasma concentration–time curve of AC1497 were, respectively 6.82- and 3.14-fold higher for SNEDDS-F4 than for the drug powder. In conclusion, SNEDDS-F4 with Capryol 90, Kolliphor RH40, and Transcutol HP (20:45:35, w/w) effectively improves the solubility and oral absorption of AC1497.

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Overcoming multidrug resistance by a combination of chemotherapy and photothermal therapy mediated by carbon nanohorns

Journal of Materials Chemistry B ◽

10.1039/c6tb01469k ◽

2016 ◽

Vol 4 (36) ◽

pp. 6043-6051 ◽

Cited By ~ 17

Author(s):

Junling Wang ◽

Ran Wang ◽

Fangrong Zhang ◽

Yajun Yin ◽

Leixia Mei ◽

...

Keyword(s):

Drug Delivery ◽

Multidrug Resistance ◽

Drug Delivery System ◽

Delivery System ◽

Targeted Drug Delivery ◽

Photothermal Therapy ◽

Carbon Nanohorns ◽

P Glycoprotein ◽

Targeted Drug ◽

Targeted Drug Delivery System

A targeted drug delivery system based on carbon nanohorns for targeting P-glycoprotein and delivering etoposide into cells to overcome multidrug resistance.

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FORMULATION AND CHARACTERIZATION OF SELF EMULSIFYING DRUG DELIVERY SYSTEM OF SPIRONOLACTONE

Asian Journal of Pharmaceutical Research and Development ◽

10.22270/ajprd.v7i1.462 ◽

1970 ◽

Vol 7 (1) ◽

pp. 38-40

Author(s):

Ankur Gupta ◽

Arpna Indurkhya ◽

S.C Chaturvedi ◽

Ajit Varma

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Oral Absorption ◽

Tween 80 ◽

Water Soluble ◽

Absolute Bioavailability ◽

Polyethylene Glycol 400

Spironolactone is aldosterone antagonist drug belonging to the category of potassium sparing diuretics administered orally that has absolute bioavailability of only 68% due to the poor aqueous solubility. The main aim of the present work was to develop a self emulsifying drug delivery system (SEDDS) to enhance the oral absorption of spironolactone. The solubility of spironolactone in various oils, surfactants, and co surfactants was determined. Pseudo ternary phase diagrams were constructed using castor oil, Tween 80, and polyethylene glycol 400, and distilled water to identify the efficient self-micro emulsion region. Prepared self emulsifying drug delivery system was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro drug release. The results showed that 96.16% drug was released from the SEDDS formulation in 3 hrs. This demonstrated an enhancement in the drug release and thereby, absorption of the drug through the membrane, this was significantly higher than that of the plain drug suspension. Thus, the above findings support that the utility of SEDDS to enhance solubility and dissolution of poorly water soluble compounds which may result in improved Therapeutic performance.

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Mechanism of enhanced oral absorption of akebia saponin D by a self-nanoemulsifying drug delivery system loaded with phospholipid complex

Drug Development and Industrial Pharmacy ◽

10.1080/03639045.2018.1526183 ◽

2018 ◽

Vol 45 (1) ◽

pp. 124-129 ◽

Cited By ~ 5

Author(s):

Yuhui Wang ◽

Jinyang Shen ◽

Xiaolin Yang ◽

Ye Jin ◽

Zhonglin Yang ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Absorption ◽

Phospholipid Complex

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Self Emulsifying Drug Delivery System: A Recent Approach

Asian Journal of Chemistry ◽

10.14233/ajchem.2019.21569 ◽

2019 ◽

Vol 31 (4) ◽

pp. 751-759 ◽

Cited By ~ 1

Author(s):

Sabitri Bindhani ◽

S. Mohapatra ◽

R.K. Kar

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability ◽

Oral Absorption ◽

Scale Up ◽

Aqueous Solubility ◽

Oral Drug ◽

Recent Approach ◽

Poorly Soluble

In recent years, nearly 40 % newer drugs compounds are hydrophobic in nature, which is a major challenge now-a-days for oral drug delivering due to low aqueous solubility. Lipid based drug delivery system is one of the favourable approach for poorly soluble compounds which can improve the drug absorption and oral bioavailability. Due to ion-pairing with appropriate surfactant and co-surfactant the macromolecular drug molecular oil droplet being found in the gut flow oral absorption which sufficiently stable towards lipase. Due to the formation of emulsified drug in micron level, it can efficiently endow the oral bioavailability. Several comprehensive papers have been published in the literature illustration diverse type of lipid based formulation with recent advancements. This article is based on an exhaustive and updated review on newer technology which out line an explicit discussion on its formulations and industrial scale up.

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Formulating a single thioether-bridged oleate prodrug into a self-nanoemulsifying drug delivery system to facilitate oral absorption of docetaxel

Biomaterials Science ◽

10.1039/c8bm00947c ◽

2019 ◽

Vol 7 (3) ◽

pp. 1117-1131 ◽

Cited By ~ 1

Author(s):

Weiping Cui ◽

Shenwu Zhang ◽

Hanqing Zhao ◽

Cong Luo ◽

Bingjun Sun ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Absorption ◽

Lymphatic Transport

Single thioether-bridged oleate prodrug (DTX-S-OA) efficiently incorporated into SNEDDS can avoid P-gp efflux, facilitate lymphatic transport and thus improve bioavailability.

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