Physicochemical characterization and<i>in vivo</i>evaluation of solid self-nanoemulsifying drug delivery system for oral administration of docetaxel

Quan, Qi-Zhe; Kim, Dong-Wuk; Marasini, Nirmal; Kim, Dae Hwan; Kim, Jin Ki; Kim, Jong Oh; Yong, Chul Soon; Choi, Han‐Gon

doi:10.3109/02652048.2012.726280

Cited by 23 publications

(9 citation statements)

References 29 publications

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“…Solubility screening of DCT has been reported with several excipients, of which Capryol 90 and Transcutol HP showed the highest solubility612. In our study, DCT also showed higher solubility in Transcutol HP and Capryol 90, thus these were selected as appropriate co-surfactants and oil, respectively for the development of D-SEDDS.…”

Section: Discussionsupporting

confidence: 51%

“…Several commonly used excipients in SEDDS such as Cremophor, Tween 80, Labrasol and Transcutol HP could inhibit the function of P-gp mediated drug efflux 6 9 10 11 . Capryol 90 (Polyethylene glycol monocaprylate) and Transcutol (Diethylene glycol monoethyl ether) lead to better solubilization of DCT compared to other lipids and co-emulsifiers 6 12 . Gelucire 44/14 (PEG-32 lauric glyceride, HLB 14) and Vitamin E TPGS (Vit E TPGS) (α-Tocopherol PEG 1000 succinate) have been shown to cause highest P-gp efflux activity among all emulsifiers 13 14 15 .…”

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confidence: 99%

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Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity

Valicherla

Dave

Syed

et al. 2016

Sci Rep

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Poor bioavailability of Docetaxel (DCT) arising due to its low aqueous solubility and permeability limits its clinical utility. The aim of the present study was to develop DCT loaded self-emulsified drug delivery systems (D-SEDDS) and evaluate its potential ability to improve the oral bioavailability and therapeutic efficacy of DCT. D-SEDDS were characterized for their in vitro antitumor activity, in situ single pass intestinal perfusion (SPIP), bioavailability, chylomicron flow blocking study and bio-distribution profile. The D-SEDDS were prepared using Capryol 90, Vitamin E TPGS, Gelucire 44/14 and Transcutol HP with a ratio of 32.7/29.4/8.3/29.6 using D-Optimal Mixture Design. The solubility of DCT was improved upto 50 mg/mL. The oral bioavailability of the D-SEDDS in rats (21.84 ± 3.12%) was increased by 3.19 fold than orally administered Taxotere (6.85 ± 1.82%). The enhanced bioavailability was probably due to increase in solubility and permeability. In SPIP, effective permeability of D-SEDDS was significantly higher than Taxotere. D-SEDDS showed 25 fold more in vitro cytotoxic activity compared to free DCT. Chylomicron flow blocking study and tissue distribution demonstrated the intestinal lymphatic transport of D-SEDDS and higher retention in tumor than Taxotere. The data suggests that D-SEDDS showed desired stability, enhanced oral bioavailability and in vitro antitumor efficacy.

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Section: Discussionsupporting

confidence: 51%

mentioning

confidence: 99%

Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity

Valicherla

Dave

Syed

et al. 2016

Sci Rep

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“…These SNEDDS produced a nanoemulsion in water and showed 12.5% absolute bioavailability as compared to a clear DTX solution given either via IV or orally. 109 Another approach used to enhance the oral bioavailability of DTX used a solid supersaturable emulsifying drug delivery system. The system showed improved oral bioavailability of DTX in rats, as revealed by an 8.77-and 1.45-fold increased area under the curve as compared to DTX and conventional SEDDS.…”

Section: Nanoemulsionsmentioning

confidence: 99%

Advancements in the oral delivery of Docetaxel: challenges, current state-of-the-art and future trends

Sohail

Rehman

Sarwar

et al. 2018

IJN

105

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The oral delivery of cancer chemotherapeutic drugs is challenging due to low bioavailability, gastrointestinal side effects, first-pass metabolism and P-glycoprotein efflux pumps. Thus, chemotherapeutic drugs, including Docetaxel, are administered via an intravenous route, which poses many disadvantages of its own. Recent advances in pharmaceutical research have focused on designing new and efficient drug delivery systems for site-specific targeting, thus leading to improved bioavailability and pharmacokinetics. A decent number of studies have been reported for the safe and effective oral delivery of Docetaxel. These nanocarriers, including liposomes, polymeric nanoparticles, metallic nanoparticles, hybrid nanoparticles, dendrimers and so on, have shown promising results in research papers and clinical trials. The present article comprehensively reviews the research efforts made so far in designing various advancements in the oral delivery of Docetaxel. Different strategies to improve oral bioavailability, prevent first-pass metabolism and inhibition of efflux pumping leading to improved pharmacokinetics and anticancer activity are discussed. The final portion of this review article presents key issues such as safety of nanomaterials, regulatory approval and future trends in nanomedicine research.

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“…Oil (Capmul MCM), surfactant (Cremophor EL) and co-surfactant (Transcutol P) were selected for L-SMEDDS. The L-SMEDDS was prepared as reported in literature [25] . Piroxicam (10 mg) was transferred into a screw-capped glass vial containing selected oil, surfactant and co-surfactant mixture (S-Cos mix in 2:1 ratio) and stirred with vortex to obtain homogenous solution.…”

Section: Formulation Of Liquid Smedds (L-smedds)mentioning

confidence: 99%

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

Pattewar¹,

Kasture²,

Pande³

et al. 2018

pharmaceutical-sciences

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The aim of present study was to formulate and evaluate self-microemulsifying drug delivery system containing piroxicam and to use the ability of porous magnesium alumina metasilicate as a solid carrier for self-microemulsifying drug delivery system. It was developed to resolve the problems of piroxicam such as low water solubility, low bioavailability and gastrointestinal irritation. Self-microemulsifying drug delivery system containing varying proportions of Capmul MCM, Cremophor EL and Transcutol-P were prepared and optimized using response surface methodology of Design-Expert ® software version 10. Liquid selfmicroemulsifying drug delivery systems were subjected to in vitro evaluation, including self-emulsification efficiency study, droplet size, zeta potential measurement and in vitro drug release studies. Solid selfmicroemulsifying drug delivery system was prepared by adding liquid self-microemulsifying drug delivery system with Neusilin US2 and filled in hard gelatin capsule. The optimized formulation consists of 28.26 % of Capmul MCM, 44.16 % of Cremophor EL and 27.58 % of Transcutol-P. The results showed that the drug release profile of piroxicam from the self-microemulsifying drug delivery formulations was higher than the pure piroxicam powder. The release of piroxicam was rapid and complete. Solid self-microemulsifying drug delivery systems after filled in hard gelatin capsule, predicted to be a promising technique to deliver a liquid formulation in solid dosage form.

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Physicochemical characterization andin vivoevaluation of solid self-nanoemulsifying drug delivery system for oral administration of docetaxel

Cited by 23 publications

References 29 publications

Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity

Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity

Advancements in the oral delivery of Docetaxel: challenges, current state-of-the-art and future trends

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

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