Optimized nanoemulsifying systems with enhanced bioavailability of carvedilol

Singh, Bhupinder; Singh, Ramandeep; Bandyopadhyay, Shantanu; Kapil, Rishi; Garg, Babita

doi:10.1016/j.colsurfb.2012.07.017

Cited by 115 publications

(62 citation statements)

References 41 publications

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“…This may ostensibly be owing to the synergistic contribution of lipid, surfactant and co-surfactant in the S-SNEDDS formulations through micellar solubilization of the drug via reduction of interfacial tension to produce the oil-in-water nanoemulsion (Pouton, 2000;Shafiq et al, 2007). The characteristic ''dip'' observed for the OPT S-SNEDDS during in vitro drug release, in all respect may be attributed to the lag-time required for liquefaction of the solid nanoemulsified system into the corresponding liquid form (Attama et al, 2003;Yuksel et al, 2003;Singh et al, 2012). In contrast, there was no such event observed for the inclusion complex and MKT during in vitro drug release studies (Figure 7).…”

Section: Discussionmentioning

confidence: 99%

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

et al. 2014

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(2015) QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance, Drug Delivery, 22:6, 765-784, DOI: 10.3109/10717544.2014 AbstractOf late, solid self-nanoemulsifying drug delivery systems (S-SNEDDS) have been extensively sought-after owing to their superior portability, drug loading, stability and patient compliance. The current studies, therefore, entail systematic development, optimization and evaluation (in vitro, in situ and in vivo) of the solid formulations of (SNEDDS) lovastatin employing rational quality by design (QbD)-based approach of formulation by design (FbD). The patient-centric quality target product profile (QTPP) and critical quality attributes (CQAs) were earmarked. Preformulation studies along with initial risk assessment facilitated the selection of lipid (i.e. Capmul MCM), surfactant (i.e. Nikkol HCO-50) and co-surfactant (i.e. Lutrol F127) as CMAs for formulation of S-SNEDDS. A face-centered cubic design (FCCD) was employed for optimization using Nikkol-HCO50 (X 1 ) and Lutrol-F127 (X 2 ), evaluating CQAs like globule size, liquefaction time, emulsification time, MDT, dissolution efficiency and permeation parameter. The design space was generated using apt mathematical models, and the optimum formulation was located, followed by validation of the FbD methodology. In situ SPIP and in vivo pharmacodynamic studies on the optimized formulation carried out in unisex Wistar rats, corroborated superior drug absorption and enhanced pharmacodynamic potential in regulating serum lipid levels. In a nutshell, the present studies report successful QbD-oriented development of novel oral S-SNEDDS of lovastatin with distinctly improved biopharmaceutical performance.

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Section: Discussionmentioning

confidence: 99%

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

et al. 2014

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“…The samples, after suitable dilution(s), were analyzed spectrophotometrically at absorption maxima. Dissolution study was also conducted on pure in an analogous manner 28 .…”

Section: Dilutability Test Processmentioning

confidence: 99%

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2017

IJPSR

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Self nano-emulsifying system drug delivery system (SNEDDS) is promising for drugs of BCS class II. The objective of present study to develop self nano-emulsifying drug delivery system for Lipophillic drug Telmisartan (antihypertensive drug), labrafil 1944, Kolliphor ELP: Span 80 (1:1) and PEG 400: Ethanol (1:1) was chosen as oil, Surfactant and Co-surfactant as they show higher solubility for Telmisartan. Screening of Surfactant, Co-surfactant done by percent transmittance and were also observed for turbidity or phase separation visually. Pseudo ternary phase diagram were constructed to identify the self emulsifying regions and also to establish the optimum concentration of oil, surfactant and co-surfactant. Box bhenken desine applied for optimization of formulation. Prepared formulation further Characterization done. Percent Drug Content found 99.71, thermodynamic stability studies show homogenous and no phase separation, Emulsifying Study performed transparent appearance after 24 hr, for robustness Dilutability in water and 0.1N HCl give Percentage Transmittance 99.5 and 100, conducting in vitro dissolution test compared with marketed preparation in stimulated gastric (S.G.F) pH 1.2 showed Percent Drug Release 93.98 with in 30 min, compared by pure drug which was 14.26. Particle size found 164.9 nm which is under nano size range, performing Poly Dispersity Index (PDI) 0.228, Zeta Potential found to be -26.0 mV, by using particle size analyzer.TEM study shows uniform spherical nano emulsion droplets. From the present study it is clear that SNEDDS can be formulated to improve the dissolution and oral bioavailability of poorly water soluble drug Telmisartan.

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“…Equilibrium solubility studies on artemether were carried out in various MCTs (namely Capmul PG 8, Captex 300 EP/NF, Captex 200, Captex 355 and Capmul MCM), LCTs (namely oleic acid, ethyl oleate, olive oil and sesame oil), surfactants (namely Tween 20, Tween 40, Tween 80, Cremophor EL, Cremophor RH40) and cosolvent (namely Transcutol HP), employing shake flask method (Beg et al, 2013;Singh et al, 2013). Briefly, an excess amount of the drug was added to different vials containing 1.0 g of each of the excipients and vortexed for 2 min to obtain the homogenous mixture.…”

Section: Equilibrium Solubility Studiesmentioning

confidence: 99%

“…The phase titration studies were carried out by water titration method for constructing the pseudoternary phase diagrams employing lipid and surfactant/co-surfactant mixtures (S mix ) in the ratios ranging between 1:9 and 9:1 (Beg et al, 2012;Singh et al, 2013). The S mix ratio of 1:0, 1:1, 2:1 and 3:1 were explored to delineate the boundaries of nanoemulsion region (Negi et al, 2015).…”

Section: Construction Of Pseudoternary Phase Diagramsmentioning

confidence: 99%

“…Currently, as per the ICH Q8 guidance, DoE is considered as one of the pivotal tool for implementing Quality by Design (QbD) for attaining product and process understanding (Yu, 2008). The practical utility of QbD approach for development of diverse drug products has been demarcated in a series of literature reports (Singh et al, 2011a;Bandyopadhyay et al, 2012;Singh et al, 2013;Beg et al, 2015a).…”

Section: Introductionmentioning

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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Optimized nanoemulsifying systems with enhanced bioavailability of carvedilol

Cited by 115 publications

References 41 publications

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

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

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