scholarly journals Formulation and Evaluation of Herbal Drug Loaded Self Nano Emulsifying Drug Delivery System (SNEDDS)

Author(s):  
Vishal N Kushare ◽  
Saravanan S

The goal of this research was to formulate and test invitro the self-nano emulsifying drug delivery system (SNEDDS) of poorly water-soluble herbal material. Linalool, an essential of Coriandrum sativum with anti-epileptic activity, was isolated from Coriandrum sativum by using Soxhlet extraction method followed by column chromatography and fractionates are concentrated under reduced pressure by using rotary flash evaporator. It is low water soluble material; unpredictable dissolution and low bioavailability make it very difficult to administer linalool orally.The captex-200 oil was exhibited maximum solubility of linalool. Thus, it was chosen as the oil phase, while Tween 80 and PEG-200 were chosen as surfactant and co-surfactant respectively for the preparation of linalool SNEDDS. For the determination of existence zone of nanoemulsion, pseudo ternary phase diagram was developed using the Prism Software by using water titration method. Self-nanoemulsion are evaluated for scanning electron microscopy (SEM), particle size analysis, polydispersity index, zeta potential and invitro drug release.The s9 formulation showed 97.72% cumulative release higher than other selected formulations(S4-S8). The S9 formulation showed promising result on droplet size, zeta potential, polydispersity index, invitro drug dissolution. It was concluded that SNEDDS formation from captex-200, tween 80, PEG-200, Smix (4:1), is a promising approach to enhancing substance solubility and the pace of dissolution.

Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.


Author(s):  
MAGFIRAH ◽  
INDAH KURNIA UTAMI

Objective: Parang romang (Boehmeria virgata) is one of the traditional medicines that are used empirically by Makassar tribal healers, South Sulawesi, as an antitumor drug. This traditional medicine contains secondary metabolites such as alkaloids, flavonoids, tannins, and saponins. However, secondary metabolites of those leaves extract have low solubility in water. Hence, to be formula, self-nanoemulsifying drug delivery system (SNEDDS) is one of the solutions to increase the extract solubility. Methods: The optimization of two formula optimum SNEDDS parang romang leaves (T80PGMZ and T20PGMZ) was using the simple lattice design (SLD) method which will give 28 SNEDDS formula parang romang leaves each of which the formula is tested for its characteristics as a critical point include emulsification time, % transmittance, drug loading, particle size, zeta potential, polydispersity index, and morphology particle. Results: The results of SNEDDS characterization obtained the optimum formula T80PGMZ with emulsification time 12.6 s, % transmittance 92.21%, drug loading 68.21 ppm, particle size 370.26 nm, zeta potential −31.4 mV, polydispersity index of 0.615, and regular particle morphology with spherical chunks at a magnification of 10,000 times with a particle size of 10 μm. Conclusion: SNEDDS of parang romang leaves extracts that used olive oil as oil phase, Tween 80 as a surfactant, and propylene glycol as the cosurfactant provided nanoemulsion with good characteristics.


1970 ◽  
Vol 7 (1) ◽  
pp. 38-40
Author(s):  
Ankur Gupta ◽  
Arpna Indurkhya ◽  
S.C Chaturvedi ◽  
Ajit Varma

Spironolactone is aldosterone antagonist drug belonging to the category of potassium sparing diuretics administered orally that has absolute bioavailability of only 68% due to the poor aqueous solubility. The main aim of the present work was to develop a self emulsifying drug delivery system (SEDDS) to enhance the oral absorption of spironolactone. The solubility of spironolactone in various oils, surfactants, and co surfactants was determined. Pseudo ternary phase diagrams were constructed using castor oil, Tween 80, and polyethylene glycol 400, and distilled water to identify the efficient self-micro emulsion region. Prepared self emulsifying drug delivery system was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro drug release. The results showed that 96.16% drug was released from the SEDDS formulation in 3 hrs. This demonstrated an enhancement in the drug release and thereby, absorption of the drug through the membrane, this was significantly higher than that of the plain drug suspension. Thus, the above findings support that the utility of SEDDS to enhance solubility and dissolution of poorly water soluble compounds which may result in improved Therapeutic performance.


2012 ◽  
Vol 62 (4) ◽  
pp. 563-580 ◽  

The aim of the study was to develop and evaluate a self- -emulsifying drug delivery system (SEDDS) formulation to improve solubility and dissolution and to enhance systemic exposure of a BCS class II anthelmetic drug, albendazole (ABZ). In the present study, solubility of ABZ was determined in various oils, surfactants and co-surfactants to identify the microemulsion components. Pseudoternary phase diagrams were plotted to identify the microemulsification existence area. SEDDS formulation of ABZ was prepared using oil (Labrafac Lipopfile WL1349) and a surfactant/ co-surfactant (Tween 80/PEG 400) mixture and was characterized by appropriate studies, viz., microemulsifying properties, droplet size measurement, in vitro dissolution, etc. Finally, PK of the ABZ SEDDS formulation was performed on rats in parallel with suspension formulation. It was concluded that the SEDDS formulation approach can be used to improve the dissolution and systemic exposure of poorly water-soluble drugs such as ABZ.


2020 ◽  
Vol 25 (2) ◽  
pp. 81
Author(s):  
Anif Nur Artanti ◽  
Fea Prihapsara ◽  
Dian Eka Ermawati ◽  
Aprilia Saefanan Shofa

Soursop leaf chloroform extract has anticancer activity.  The active ingredient of soursop leaf was acetogenin polypoid derivatives that have a lipophilic characteristic, and less effective to achieve action targets of drugs in biological systems. The Self-Micro Emulsifying Drug Delivery System (SMEDDS) was an effective drug delivery technique that increases the solubility of lipophilic drugs. This study aims to determine the proportion of optimum SMEDDS formula using Simplex Lattice Design (SLD) method. The Formula of SMEDDS was prepared using a combination of Tween 80-Croduret, Propylene Glycol, and Candlenut oil. Optimization formula with SLD method using Design-Expert software based on physical stability parameters there are the percent of transmittance and emulsification time. The optimum formula of SMEDDS was compared with SLD prediction formula using a statistical analysis t-test, then test of loading dose extract, stability test accelerated by centrifugation, particle size, and zeta potential. The proportion of optimum composition of Tween 80-Croduret, Propylene Glycol, and Candlenut oil of SMEDDS was 60.87%; 24.13%; 15.00% respectively. Results of transmittance 41.14±3.78% and emulsification time 119.0±2.08 seconds. The predicted SLD value for the transmittance percent was 55.0% and the emulsification time was 119.59 seconds. The result of the statistical analysis of one sample t-test showed no significant difference between observation results and SLD prediction. The SMEDDS system has F value of 0.99 and capable to load 25.0 mg chloroform extract of soursop leaf each system with an average particle size of 440 nm and zeta potential of +21.5 mV. 


Author(s):  
JAMEER A TAMBOLI ◽  
SHRINIVAS K MOHITE

Objective: The objective of the present study was to develop solid self-microemulsifying drug delivery system (S-SMEDDS) of diacerein (DCN) for enhancement of dissolution rate. Methods: Three batches of liquid SMEDDS were prepared using oleic acid, Tween 80, and polyethylene glycol 200 as oil, surfactant, and cosurfactant, respectively. Microemulsion region was recognized by constructing a pseudoternary phase diagram containing a different proportion of oil, surfactant, and cosurfactant. Prepared liquid SMEDDS was evaluated for thermodynamic stability study, dispersibility tests, globule size, zeta potential, and viscosity. Liquid SMEDDS was then converted to S-SMEDDS by adsorption technique using Neusilin US2 as a solid carrier. Prepared S-SMEDDS was evaluated for different micromeritic properties, drug content, reconstitution properties, in vitro dissolution study, Fourier transform infrared, and scanning electron microscopy. Results: The results showed that all batches of liquid SMEDDS were found to be thermodynamically stable. Reconstitution properties of S-SMEDDS showed spontaneous microemulsification with globule size 0.271 μm and −16.18 mV zeta potential. From the results of in vitro dissolution study, it was found that the release of DCN was significantly increased as compared with plain DCN. Conclusion: The study concluded that dissolution rate of poorly water-soluble drug like DCN can be increased by developing S-SMEDDS formulation.


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Shailesh T. Prajapati ◽  
Harsh A. Joshi ◽  
Chhaganbhai N. Patel

Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro dissolution, and in vitro and ex vivo drug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release. The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.


Molecules ◽  
2015 ◽  
Vol 20 (8) ◽  
pp. 14684-14698 ◽  
Author(s):  
Marko Krstić ◽  
Miljana Popović ◽  
Vladimir Dobričić ◽  
Svetlana Ibrić

Author(s):  
Zainab Ali Hussein

Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes ,the oral bioavailability is  approximately 6%, therefore aim  its  prepare and evaluate bromocriptine mesylate  as liquid self nano emulsifying drug delivery system to enhance its solubility , dissolution and stability . Solubility study was made in different vehicles to select the best excipients for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios of surfactant and co-surfactant, four formulations were prepared using various concentrations of castor oil, tween 80 and ethanol. All prepared formulations were evaluated for particle size distribution, polydispersity index, drug content, thermodynamic stability, dispersibility and emulsification time, robustness to dilution and in vitro drug dissolution. It was found that release rate and extent for all prepared formulations were significantly higher (p < 0.05) than plain drug powder. from the study, it was concluded that self-nanoemulsifying drug delivery system is a promising approach to improve solubility, dissolution, and stability of bromocriptine mesylate.


This work reported a first liquid self-nanoemulsifying drug delivery system (SEDD) of cilostazol using oleic acid as oil phase, tween 80 as surfactant, and transcutol as co-surfactant. Cilostazol is a poor water-soluble phosphodiesterase III inhibitor, which has antiplatelet and vasodilator effect used to relief intermittent claudication symptoms. Cilostazol solubility was determined in various oils, surfactants and co-surfactants and phase diagram was constructed at different oil: surfactant: co-surfactant ratios to determine the existence of nano-emulsion region. The in-vitro dissolution profile showed an optimized cilostazol SEDD formula (LT1) containing oleic acid (10%) as oil, tween 80 (45%) as surfactant, and transcutol (45%) as co-surfactant in comparison with the commercial conventionally Tablets. The LT1 formula was thermodynamically sTable, with a zeta potential of -30.48 mV and droplet size 154 nm. The LT1 capsule showed a superior dissolution profile (100%) when compared to the commercial Tablet (64%) of cilostazol. The objective of the present study is to formulate cilostazol as an oral liquid SEDD with better solubility and drug release to overcome a variable bioavailability of the commercial Tablet in which a high-fat meal increases absorption to approximately 90%.


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