Formulation and Evaluation of Self-Nanoemulsifying Drug Delivery System of Naproxen

2015 ◽  
Vol 8 (1) ◽  
pp. 2715-2722
Author(s):  
Saritha D ◽  
Penjuri Subhash Chandra Bose ◽  
Nagaraju Ravoru
Keyword(s):  
Drug Delivery ◽  
Oral Administration ◽  
Drug Delivery System ◽  
Delivery System ◽  
Water Soluble ◽  
Size Analysis ◽  
Albino Rats ◽  
Significant Activity ◽  
Water Soluble Drugs

Self-emulsifying drug delivery systems (SEDDS) possess unparalleled potential in improving oral bioavailability of poorly water-soluble drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro or nanoemulsions containing the solubilized drug. The objective of the present work was to formulate a self nanoemulsifying drug delivery system (SNEDDS) for naproxen. Naproxen SNEDDS were formulated using Labrafac PG (Oil), Span 80 (Surfactant) and propylene glycol (Co surfactant). The developed SNEDDS were evaluated for turbidimetry, droplet size analysis, zeta potential, refractive index, viscosity, drug content and in vitro diffusion profiles. All formulations of naproxen SNEDDS showed globule size in nanometric range, good stability with no phase separation and rapidly formed clear emulsion. All formulations showed more than 95% of drug release at the end of 60 min. The SEDDS showed improved dissolution rate compared to pure naproxen. Anti-inflammatory studies were conducted in Wistar strain male albino rats and ibuprofen SNEDDS showed more significant activity than the pure drug. The study illustrated the potential of naproxen SNEDDS for oral administration and its biopharmaceutical performance.

scholarly journals Development of a self-microemulsifying drug delivery system of domperidone: In vitro and in vivo characterization

2013 ◽  
Vol 63 (2) ◽  
pp. 241-251 ◽  
Author(s):  
Ramesh Jakki ◽  
Muzammil Afzal Syed ◽  
Prabhakar Kandadi ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Ternary Phase Diagram ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Size Analysis

The main objective of this work was to prepare a self-micro emulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of domperidone, a poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. The in vitro self-micro emulsification properties and droplet size analysis of SMEDDS were studied following their addition to water under mild agitation. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions (1:100, 1:500, 1:1000) and freeze-thaw stability. The optimized formulation, SMEDDS-B used for in vitro dissolution and bioavailability assessment, contained oil (Labrafac CC, 25 %, m/m), surfactant (Tween 80, 55 %, m/m), and co-surfactant (Transcutol®, 20 %, m/m). The preliminary oral bioavailability of domperidone from SMEDDS was 1.92-fold higher compared to that of domperidone suspension in rats. The AUC0-24 and cmax values were 3.38 ± 0.81 μg h mL-1 and 0.44 ± 0.03 μg mL-1 for SMEDDS-B formulation in comparison with 1.74 ± 0.18 μg h mL-1 and 0.24 ± 0.02 μg mL-1 for domperidone suspension, suggesting a significant increase (p < 0.05) in oral bioavailability of domperidone from SMEDDSS.

scholarly journals Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

2012 ◽  
Vol 62 (4) ◽  
pp. 563-580 ◽  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Systemic Exposure ◽  
Tween 80 ◽  
Water Soluble ◽  
Formulation Development ◽  
Suspension Formulation ◽  
Water Soluble Drugs

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.

Formulation and Evaluation of Solid Self-Nanoemulsifying Drug Delivery System for Enhancing the Solubility and Dissolution Rate of Budesonide

2021 ◽  
pp. 5755-5763
Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Water Soluble ◽  
Drug Release Profile ◽  
Water Soluble Drug

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.

DEVELOPMENT AND EVALUATION OF ZIPRASIDONE LOADED SOLID SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 53-60
Author(s):  
Purushottam Patil ◽  
Malik Shaikh ◽  
Paresh Mahaparale
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Physical Adsorption ◽  
Gastrointestinal Transit ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Poorly Water Soluble

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone.

Preparation and Evaluation of Chitosin-Coated Alginate/Gelatin Microspheres for Sustained-Release Drug Delivery System In Vitro

2013 ◽  
Vol 651 ◽  
pp. 227-231
Author(s):  
Qiang Song Wang ◽  
Yuan Lu Cui ◽  
Tian Jiao Dong
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Water Soluble ◽  
Average Particle ◽  
Gelatin Microspheres ◽  
Release Drug ◽  
Ft Ir

The purpose of the study was to prepare and evaluation chitosin-coated alginate/gelatin microspheres for sustained-release drug delivery system in vitro. The microspheres were prepared with an emulsification technique, characterized by scanning electron microscopy (SEM), Fourier transform infrared spectrophotometry (FT-IR), differential scanning calorimetry (DSC). The average particle size of the chitosan-coated alginate/gelatin microspheres was uniform. The results of FT-IR and DSC showed that the microspheres were formed by intermolecular cross-linkages between chitosan and gelatin. The results also implied that the microsphere were a practicable dosage form to increase drug loading ratio for the poorly water-soluble drugs by encapsulated with chitosan. In vitro release of the microsphere indicated that it had a satisfactory sustained-release behavior for the sustained-release drug delivery system.

scholarly journals FORMULATION AND CHARACTERIZATION OF SELF EMULSIFYING DRUG DELIVERY SYSTEM OF SPIRONOLACTONE

1970 ◽  
Vol 7 (1) ◽  
pp. 38-40
Author(s):  
Ankur Gupta ◽  
Arpna Indurkhya ◽  
S.C Chaturvedi ◽  
Ajit Varma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Absorption ◽  
Tween 80 ◽  
Water Soluble ◽  
Absolute Bioavailability ◽  
Polyethylene Glycol 400

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.

scholarly journals Formulation and In-vitro evaluation of liposomal drug delivery system of metformin HCl

2019 ◽  
Vol 9 (2) ◽  
pp. 31-37
Author(s):  
Subbramanian L ◽  
M Anitha Rani ◽  
T Rajasekaran ◽  
M Ramanathan ◽  
P Solairaj
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Morphological Analysis ◽  
Size Analysis ◽  
Dispersion Method ◽  
Injection Method ◽  
Soya Lecithin ◽  
Metformin Hcl

Metformin is widely used for the treatment of diabetes; the intention of the present study was to formulate Metformin HCl liposomes for a sustained drug delivery system. It have the advantages of dose reduction, less dosing frequency, minimize the side effect, prolong the action of drug and thus achieve better patient compliance. The liposomes were prepared by physical dispersion and ether injection method. Soya lecithin and cholesterol were used for encapsulating the drug, it facilitates to release the medicaments in sustained manner. Chloroform, ether and methanol were used as a solvent. Phosphate buffer pH 6.8 was used as a hydration medium for loading the drug. The final liposome was evaluated in various quality parameters of drug entrapment efficiency, morphological analysis, particle size analysis, in-vitro drug release studies and stability studies. In the two methods of metformin liposome formulation the ether injection method showed prolonged action when compared to physical dispersion method. In the parameters of drug entrapment and stability physical dispersion method was shows better results. Keywords: Physical dispersion, ether injection, soya lecithin, cholesterol, morphological analysis, metformin.

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