Self-Nanoemulsifying Drug Delivery System of Nifedipine: Impact of Hydrophilic–Lipophilic Balance and Molecular Structure of Mixed Surfactants (original) (raw)
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NANOTECHNOLOGY APPROACH-SELF NANOEMULSIFYING DRUG DELIVERY SYSTEM (SNEDDS) Review Article
International Journal of Applied Pharmaceutics, 2023
This review article aims to develop nanotechnology in novel drug delivery systems using self-nano emulsifying drug delivery systems (SNEDDS). This Article was selected using a database with Prism Guideline diagrams. A total of 18 articles obtained from 2010-2020 were used as the primary reference to be analyzed using a systematic review method in the form of meta-synthesis. This review describes the mechanism of SNEDDS in increasing absorption, the components of the SNEDDS formula, the characterization of self-nano emulsifying drug delivery systems (SNEDDS), the effect of the physicochemical properties of SNEDDS on in vivo activity, and the basis for selecting compounds in the SNEDDS formulation. Self-Nanoemulsifying Drug Delivery System (SNEDDS) is a novel drug delivery system from nanoemulsion used to increase the solubility of lipophilic drugs. SNEDDS is an isotropic mixture consisting of oil, surfactant, and co-surfactant. SNEDDS is considered pre-concentrated nanoemulsions or anhydrous forms of nanoemulsions. In SNEDDS, the formation of nanoemulsions occurs when selfnanoemulsions come into contact with gastrointestinal fluids in the presence of light stirring in the peristaltic motion of the gastrointestinal tract. In general, SNEDDS have small particle sizes in the range of 10-200 nm. The application of the self nanoemulsion development system can be used for BCS Class II lipophilic drug compounds and BCS Class IV drugs. SNEDDS is a novel drug delivery system that can be used for oral drug delivery. In occlusion, a self-nanoemulsifying drug delivery system (SNEDDS) is a new approach for the formulation of drug molecules with poor water solubility. Self Nanoemulsifying drug delivery system (SNEDDS) is an isotropic mixture of oil, surfactant, and co-surfactant.
International Journal of Applied Pharmaceutics, 2020
Objective: The objective of this work was to improve the solubility and dissolution rate of Nifedipine by preparing a solid-self micro emulsifying drug delivery system (Solid-smedds). Methods: Liquid-self-emulsifying drug delivery system formulations were prepared by using linseed oil as oil, tween 80 as a surfactant and PEG 400 as cosurfactant. Components were selected by solubility screening studies and the self-emulsifying region was identified by the pseudo-ternary phase diagram. Thermodynamic stability study was performed for the determination of stable liquid-smedds formulation. These formulations were evaluated for self-emulsification time, drug content analysis, robustness to dilution test, particle size analysis, in vitro diffusion study, and Stability study. Solid self-micro emulsifying formulations were prepared by using aerosil-200 at a different ratio. Lf9S (0.65:1) was selected due to its highest drug entrapment efficiency and a decrease in particle size. It was select...
Pharmaceutical Nanotechnology, 2014
Nebivolol HCl (NBL) a third generation beta blocker poses lack of oral bioavailability (12%) owing to its low solubility and first pass biotransformation in liver. The present research was undertaken to prepare solid Selfnanoemulsifying drug delivery system (S-SNEDDS) of NBL which will present NBL at molecular level in nanoemulsion form throughout GIT. Increased solubility along with intestinal lymphatic transport of lipid rich nanoemulsified drug bypassing hepatic first pass may enhance bioavailability. Based on solubilization of the drug and spontaneity of selfemulsification, Peceol as an oily phase, Cremophore RH 40 and Gelucire 50/13 as surfactants and ethanol as cosurfactant/co-solvent were selected as the excipients to produce NBL loaded S-SNEDDS. Total 9 formulations were made with different ratios of the excipients and the optimized formulation was selected on the basis of solidification of SNEDDS on refrigeration and maintenance of the solid state. Spherical shaped morphology of oil globules was confirmed by TEM analysis. On dilution S-SNEDDS showed nanoparticles of size 180-190nm with a Polydispersity index 0.4-0.8 and Zeta potential-5.17,-7.56mV. The DSC and X-ray diffraction patterns of the S-SNEDDS show the amorphous state of NBL in the lipid matrix. Developed S-SNEDDS showed pH-independent drug dissolution which in SIF was fourfold greater as compared to plain drug. The intestinal permeability by everted sac technique showed threefold increase in transportation of NBL from S-SNEDDS formulation compared to NBL solid suggesting that S-SNEDDS of NBL is an excellent and practical approach of enhancing the oral bioavailability through improved solubility.
2017
Developments in recent drug discovery programs, yields a large proportion of novel pharmacologically active molecules that are lipophilic and poorly soluble ,which is a major challenge for pharmaceutical researchers to enhance the oral bioavailability of such drug molecules. Compared to conventional oral dosage forms, Self nanoemulsifying drug delivery systems (SNEDDS) possesses potential advantages like ease of manufacture and scale up, quick onset of action, reduction in drug dose, reduction in inter and intra subject variability and food effects and minimize problems associated with filling of liquid SNEDDS in capsules. Several recent works on Self nanoemulsifying drug delivery systems suggests the commercial suitability of the system in improving the solubility and bioavailability of such drugs. The physicochemical properties, drug solubilization capacity and physiological fate considerably helps in the selection of the SNEDD components. The composition of the SNEDDS can be optimized mainly with the help of phase diagrams, whereas statistical experimental design can be used for further optimization. The transition of liquid SNEDDS to solid SNEDDS has also been accomplished by researchers. Solidself nanoemulsifying drug delivery system focus on the incorporation of liquid/semisolid self nano emulsifying ingredient into solids by different solidification techniques like adsorption to solid carrier, spray drying, melt extrusion, nanoparticle technology and melt granulation. The present article gives more specification on spontaneous/rapid forming nanoemulsions or self nanoemulsifying systems for oral drug delivery by adsorption technique and gives complete information about formulation, method of preparation, characterization and application in solid dosage form of self nanoemulsifying drug delivery system.
International Journal of Applied Pharmaceutics, 2016
Objective: The main purpose of this study was to optimize the different conditions for the preparation of self-nanoemulsifying drug delivery system (SNEDDS) for both Irbesartan (IRB) and Olmesartan (OLM). Methods: Based on solubility study and emulsification efficiency, Preliminary investigations of various oils, surfactants and cosurfactants were carried out for selection of the proper SNEDDS ingredients. Pseudoternary phase diagrams were then plotted using series of concentrations to obtain optimum SNEDDS components that identify the efficient self-nanoemulsifying region. Sixteen unloaded SNEEDS formulae were prepared using Capryol 90, Cremophor RH 40 and Transcutol HP as oil, surfactant and cosurfactant respectively. The prepared SNEDDS were evaluated for self-nanoemulsification time, the effect of dilution (with different volumes at different pH values), optical clarity, viscosity, droplet size analysis as well as the polydispersity index (PDI). SNEDDS formulae were also evaluated for thermodynamic stability and zeta potential to confirm the stability of the prepared SNEDDS. Results: The results showed that the mean droplet size of all reconstituted SNEDDS was found to be in the nanometric range (<100 nm) and showed optimum PDI values. All formulae also showed rapid emulsification time, good optical clarity and found to be highly stable. Formulae with the smallest particle size, lowest emulsification time, best optical clarity and robust to dilution and pH change were selected to be loaded with IRB and OLM for further study. Conclusion: It was concluded that the prepared self-emulsified prototype was ready to incorporate many poorly soluble drugs in order to improve their solubility as well as bioavailability profile.
Journal of The Saudi Pharmaceutical Society, 2015
A solid self-nanoemulsifying drug-delivery system (solid SNEDDS) has been explored to improve the solubility and dissolution profile of glipizide. SNEDDS preconcentrate was systematically optimized using a circumscribed central composite design by varying Captex 355 (Oil), Solutol HS15 (Surfactant) and Imwitor 988 (Co-surfactant). The optimized SNEDDS preconcentrate consisted of Captex 355 (30% w/w), Solutol HS15 (45% w/w) and Imwitor 988 (25% w/w). The saturation solubility (SS) of glipizide in optimized SNEDDS preconcentrate was found to be 45.12 ± 1.36 mg/ml, indicating an improvement (1367 times) of glipizide solubility as compared to its aqueous solubility (0.033 ± 0.0021 mg/ml). At 90% SS, glipizide was loaded to the optimized SNEDDS. In-vitro dilution of liquid SNEDDS resulted in a nanoemulsion with a mean droplet size of 29.4 nm. TEM studies of diluted liquid SNEDDS confirmed the uniform shape and size of the globules. The liquid SNEDDS was adsorbed onto calcium carbonate and talc to form solid SNEDDS. PXRD, DSC, and SEM results indicated that, the presence of glipizide as an amorphous and as a molecular dispersion state within solid SNEDDS. Glipizide dissolution improved Abbreviations: solid SNEDDS, solid self-nanoemulsifying drug delivery system; SS, saturation solubility; DR 15min , percentage drug release in 15 minutes; LCT, long chain triglycerides; MCT, medium chain triglycerides.
ABSTRACT Introduction: Lipid-based drug delivery systems (LBDDS) are the most promising technique to formulate the poorly water soluble drugs. Nanotechnology strongly influences the therapeutic performance of hydrophobic drugs and has become an essential approach in drug delivery research. Self-nanoemulsifying drug delivery systems (SNEDDS) are a vital strategy that combines benefits of LBDDS and nanotechnology. SNEDDS are now preferred to improve the formulation of drugs with poor aqueous solubility. Areas covered: The review in its first part shortly describes the LBDDS, nanoemulsions and clarifies the ambiguity between nanoemulsions and microemulsions. In the second part, the review discusses SNEDDS and elaborates on the current developments and modifications in this area without discussing their associated preparation techniques and excipient properties. Expert opinion: SNEDDS have exhibit the potential to increase the bioavailability of poorly water soluble drugs. The stability of SNEDDS is further increased by solidification. Controlled release and supersaturation can be achieved, and are associated with increased patient compliance and improved drug loads, respectively. Presence of biodegradable ingredients and ease of large-scale manufacturing combined with a lot of 'drug-targeting opportunities' give SNEDDS a clear distinction and prominence over other solubility enhancement techniques.
Journal of Advanced Scientific Research
In recent years, much attention has been paid to solid self-nanoemulsifying drug delivery systems (S-SNEDDS), which have shown reasonable successes in improving oral bioavailability of poorly soluble drugs. This drug delivery system combines the advantages of liquid SNEDDS with those of a solid dosage form and overcomes the limitations associated with liquid formulations. One optimized SNEDDS formulae F-5 were selected to be solidified by spray drying technique using Aerosil 200 as solid carrier. Characterization of GOZ Loaded S-SNEDDS by angle of repose of the one S-SNEDDS formulae F-5 were 24.12°± 1.10°, these values indicate that all formulae have good flow ability. The bulk density of the two formulae F-5 was found to be 0.47 ± 0.03 g/mL. However, tapped density was 0.57±0.02 g/mL for formula F-5. Carr’s index of formulae F-5 was found to be 13.57±1.09 which give an indication about the good flowability of the one S-SNEDDS formulae. The efficiency of self-emulsification can also...
Spontaneous Emulsification of Nifedipine-Loaded Self-Nanoemulsifying Drug Delivery System
AAPS PharmSciTech, 2014
Self-nanoemulsifying drug delivery system (SNEDDS) can be used to improve dissolution of poorly water-soluble drugs. The objective of this study was to prepare SNEDDS by using ternary phase diagram and investigate their spontaneous emulsifying property, dissolution of nifedipine (NDP), as well as the pharmacokinetic profile of selected SNEDDS formulation. The results showed that the composition of the SNEDDS was a great importance for the spontaneous emulsification. Based on ternary phase diagram, the region giving the SNEDDS with emulsion droplet size of less than 300 nm after diluting in aqueous medium was selected for further formulation. The small-angle X-ray scattering curves showed no sharp peak after dilution at different percentages of water, suggesting non-ordered structure. The system was found to be robust in different dilution volumes; the droplet size was in nanometer range. In vitro dissolution study showed remarkable increase in dissolution of NDP from SNEDDS formulations compared with NDP powders. The pharmacokinetic study of selected SNEDDS formulation in male Wistar rats revealed the improved maximum concentration and area under the curve. Our results proposed that the developed SNEDDS formations could be promising to improve the dissolution and oral bioavailability of NDP.