Role of Alternative Lipid Excipients in the Design of Self-Nanoemulsifying Formulations for Fenofibrate: Characterization, in vitro Dispersion, Digestion and ex vivo Gut Permeation Studies

Nanoemulsion drug delivery systems are advanced modes for delivering and improving the bioavailability of hydrophobic drugs and the drug which have high first pass metabolism. The nanoemulsion can be prepared by both high energy and low energy methods. High energy method includes high-pressure homogenization, microfluidization, and ultrasonication whereas low energy methods include the phase inversion emulsification method and the self-nanoemulsification method. Low energy methods should be preferred over high energy methods as these methods require less energy, so are more efficient and do not require any sophisticated instruments. However high energy methods are more favorable for food grade emulsion as they require lower quantities of surfactant than low energy methods. Techniques for formulation of nanoemulsion drug delivery system are overlapping in nature, especially in the case of low energy methods. In this review, we have classified different methods for formulation of nanoemulsion systems based on energy requirements, nature of phase inversion, and self-emulsification.

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“…Self-nanoemulsification techniques (Alshamsan et al, 2018). SNEDDS, self-nanoemulsifying drug delivery system; GIT, gastrointestinal tract.…”

Section: Figmentioning

confidence: 99%

Techniques for Formulation of Nanoemulsion Drug Delivery System: A Review

Kumar

Bishnoi

Shukla

et al. 2019

pnf

293

120

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“…Changing the limit of solubilization that emerged all through this procedure was of incredible importance to assess food impact by methods of in vitro lipolysis. 62 During this study, it was very important to establish whether there was some possibility of precipitation of drug within 30 minutes. The fasted condition outcomes authenticated that rosuvastatin existed in the solubilized form in SNEDDS that resulted in about 98.32±0.05% drug discharge.…”

Section: Dovepressmentioning

confidence: 99%

“…At periodic times, test samples were expelled and assessed for physical appearance, % drug discharge, and time of disintegration. 62,63 Pharmacodynamic Investigation It has been reported that rosuvastatin has dose-dependent pharmacodynamic impact and that is the reason for the execution of this in vivo investigation with a marketed tablet.…”

mentioning

confidence: 99%

Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation

Verma¹,

Kaushik²,

Almeer³

et al. 2021

IJN

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The purpose of this proposed research was to investigate a nano-formulation developed using self-nanoemulsifying drug delivery system (SNEDDS) to improve the pharmacodynamic potential of rosuvastatin by assisting its transportation through lymphatic circulation. Methods: The utilized lipids, surfactants, and co-surfactants for SNEDDS were selected on the basis of solubility studies. The SNEDDS formulation was optimized by implementing a D-optimal mixture design, wherein the effect of concentration of Capmul MCM EP (X 1), Tween 20 (X 2) and Transcutol P (X 3) as independent variables was studied on droplet size (Y 1), % cumulative drug release (Y 2) and self-emulsification time (Y 3) as dependent variables. The optimized formulation was evaluated via in vitro parameters and in vivo pharmacodynamic potential in Wistar rats. Results: The D-optimal mixture design and subsequent ANOVA application resulted in the assortment of the optimized SNEDDS formulation that exhibited a droplet size of nano range (14.91nm), in vitro drug release of >90% within 30 minutes, and self-emulsification time of 16 seconds. The in vivo pharmacodynamic study carried out using Wistar rats confirmed the better antihyperlipidemic potential of developed formulation in normalizing the lipidic level of serum in contrast to pure drug and marketed tablets. Conclusion: This research reports the application of D-optimal mixture design for successful and systematic development of rosuvastatin-loaded SNEDDS with distinctly enhanced in vitro and in vivo performance in comparison to marketed formulation. Eventually, improved anti-hyperlipidemic efficacy was envisaged which might be attributed to increased drug solubility and absorption. Overall, this study shows the utility of SNEDDS for improving the dissolution rate and bioavailability of poor aqueous-soluble drugs. The present SNEDDS formulation could be a promising approach and alternative to conventional dosage form.

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“…During lipolysis, production of fatty acids (FAs) results in an elevation in pH of biorelevant media, 0.2 M NaOH solution was utilized for maintaining pH. The progress of drug release in digestion buffers was monitored directly by UV analysis at 254 nm (Williams et al, 2012;Alshamsan et al, 2018). By following this protocol, the present strategy was seen as robust and estimated values were reproducible.…”

Section: Robustness To Dilution Robustness Was Investigatedmentioning

confidence: 99%

“…Alterations in solubilization capacity that arises throughout this process were of great significance to evaluate food effects through in vitro lipolysis (Alshamsan et al, 2018). During this investigation, it was vital to examine if there was any chance of precipitation of medicament or loss of medicament arising within 30 min.…”

Section: Assessment Of Food Effect With Dynamic In Vitro Lipolysismentioning

confidence: 99%

Design and optimization of candesartan loaded self-nanoemulsifying drug delivery system for improving its dissolution rate and pharmacodynamic potential

Verma

Kaushik

2020

Drug Delivery

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During the last decades, much attention has been focused on SNEDDS approach to resolve concerns of BCS II class drugs with accentuation on upgrading the solubility and bioavailability. The present hypothesis confirms the theory that SNEDDS can reduce the impact of food on Candesartan solubilization, thereby offering the potential for improved oral delivery without co-administration with meals. The present studies describe quality-by-design-based development and characterization of Candesartan loaded SNEDDS for improving its pharmacodynamic potential. D-optimal mixture design was used for systematic optimization of SNEDDS, which showed globule size of 13.91 nm, more rapid drug release rate of >90% in 30 min and 16 s for self-emulsification. The optimized formulations were extensively evaluated, where an in vitro drug release study indicated up to 1.99-and 1.10-fold enhancement in dissolution rate from SNEDDS over pure drug and marketed tablet. In vivo pharmacodynamic investigation also showed superior antihypertensive potential of SNEDDS in normalizing serum lipid levels as compared to pure drug and marketed tablet that was executed on male Wistar rats. Overall, this paper reports successful systematic development of candesartan-loaded SNEDDS with distinctly improved biopharmaceutical performance. This research work interpreted a major role of SNEDDS for enhancing the rate of dissolution and bioavailability of poorly water soluble drugs.

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Role of Alternative Lipid Excipients in the Design of Self-Nanoemulsifying Formulations for Fenofibrate: Characterization, in vitro Dispersion, Digestion and ex vivo Gut Permeation Studies

Cited by 19 publications

References 30 publications

Techniques for Formulation of Nanoemulsion Drug Delivery System: A Review

Techniques for Formulation of Nanoemulsion Drug Delivery System: A Review

Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation

Design and optimization of candesartan loaded self-nanoemulsifying drug delivery system for improving its dissolution rate and pharmacodynamic potential

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