Stable drug encapsulation in micelles and microemulsions

Narang, Ajit S.; Delmarre, David; Gao, Danchen

doi:10.1016/j.ijpharm.2007.08.057

Cited by 359 publications

(221 citation statements)

References 76 publications

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“…The studies were also conducted for exploring the effect of increase in the amount of Cremophor RH40 in the S mix ratio of 1:1, 2:1 and 3:1 revealed further increase in the nanoemulsion region in 1:1 and 2:1 ratios, followed by a reduction in the ratio of 3:1 (Figure 1B-D). This can be attributed to the nonionic nature of the Cremophor RH40, which undergoes precipitation of the polyoxyethylene chains upon coming in contact with Transcutol HP during phase titration studies (Narang et al, 2007). Analogously, the pseudoternary phase titration studies conducted for identifying the apt ratio of ethyl oleate, Tween 80 and Transcutol HP for formulating the LCT-SNEDDS also revealed identical observations (Figure 2A), where the 2:1 ratio exhibited the highest area for nanoemulsion region without formation of any microgel region ( Figure 2B).…”

Section: Resultsmentioning

confidence: 99%

“…The increase in the ratio of cosolvent (i.e., Transcutol HP), however, shows drastic reduction in the nanoemulsion region, as is evident from Figure (1C and 2C). This can be explained owing to the lower HLB value (i.e., 4.2) of Transcutol HP, which reduces emulsification efficiency for forming oil-inwater microemulsion (Narang et al, 2007). In a nutshell, among the various combinations of lipid and emulsifying agents explored, the ratios of 1:1 and 2:1 were selected for formulation optimization studies of MCT and LCT-SNEDDS, respectively.…”

Section: Resultsmentioning

confidence: 99%

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Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

et al. 2016

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The current studies entail systematic development of self-nanoemulsifying drug delivery systems (SNEDDS) containing medium-chain triglycerides (MCTs) and long-chain triglycerides (LCTs) for augmenting the biopharmaceutical performance of artemether. Equilibrium solubility and pseudoternary phase diagram studies facilitated selection of Captex 355 and Ethyl oleate as MCTs and LCTs, and Cremophor RH 40 and Tween 80 as surfactants, while Transcutol HP as cosolvent for formulating the SNEDDS. Systematic optimization was performed employing the Box-Behnken design taking concentrations of lipid, surfactant and cosolvent as the critical material attributes (CMAs), while evaluating for globule size, emulsification time, dissolution efficiency and permeation as the critical quality attributes (CQAs). In situ single pass intestinal perfusion (SPIP) studies in Wistar rats substantiated significant augmentation in the absorption (5-to 6-fold) and permeation (4-to 5-fold) parameters from the optimized MCT and LCT-SNEDDS vis-à-vis the pure drug. In vivo pharmacodynamic studies in Plasmodium berghi infected laca mice exhibited superior reduction in the levels of percent parasitemia, SGOT, SGPT and bilirubin, followed by higher survival rate of the animals by optimized MCT-SNEDDS followed by LCT-SNEDDS vis-à-vis the pure drug, which was subsequently ratified through histopathological examination of liver tissues. Overall, the studies construed successful development of the optimized SNEDDS of artemether with distinctly improved biopharmaceutical and antimalarial potential.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

et al. 2016

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“…The main challenge for the formulation scientist has been the formulation and development of poorly water soluble moieties [2][3][4][5]. The lipid based formulation methodology has seen wide range of interest in improving the oral bioavailability and the drug solubilisation in the Gastrointestinal Tract (GIT) of BCS class II and IV drugs [6][7][8][9]. Current investigations support the usage of lipid based formulations to tackle the formulation challenges of poorly soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

Artesunate Loaded Self Nanoemulsified Drug Delivery System: A Preliminary Study for Improved Efficacy in the Treatment of Malaria: Formulation, Characterization and Bio-Distribution Study

R¹

2017

J Bioequiv Availab

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“…Furthermore, the opening of tight junctions facilitates paracellular transport. Drug absorption is also improved by the inhibition of efflux pumps such as P-gp [7,8].…”

Section: Introductionmentioning

confidence: 99%

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

Sisinthy

Nalamolu

Sarah

2016

Int J Pharm Pharm Sci

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Objective: The objective of the present study was to design, optimise and characterise self nano emulsifying drug delivery systems (SNEDDS) for a poorly water soluble drug, olmesartan medoxomil (OLM) by Formulation by Design (FbD) approach with an aim to improve its solubility and dissolution. Methods:The SNEDDS were systematically optimised using three factor Box-Behnken Results: Following optimisation, the values of formulation variables were found to be 142.276 mg (Capryol P), 399.999 mg (Cremophor EL) and 598.871 mg (Transcutol P) which produced a globule size of 12.64 nm, percentage drug release of 93.34% and a turbidity of 0.02 FNU. TEM studies demonstrated spherical droplet morphology.design. Concentration of formulation variables, namely, the oil phaseX1 (Capryol 90), the surfactant X2 (Cremophor EL), and the co-surfactant X3 (Transcutol P), was optimized for its impact on mean globule size (Y1), percentage drug release in 20 min (Y2) and turbidity (Y3) of the formulation. Ternary phase diagrams were constructed to select the areas of nanoemulsion and the amounts of oil, surfactant and cosurfactants as critical formulation variables. The prepared SNEDDS were characterised for globule size, dissolution studies, turbidity, and transmission electron microscopy (TEM). Conclusion:Thus, the present studies reveal that the SNEDDS is a promising drug delivery system approach for the enhancement of solubility and dissolution rate of OLM.

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Stable drug encapsulation in micelles and microemulsions

Cited by 359 publications

References 76 publications

Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential

Artesunate Loaded Self Nanoemulsified Drug Delivery System: A Preliminary Study for Improved Efficacy in the Treatment of Malaria: Formulation, Characterization and Bio-Distribution Study

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

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