scholarly journals Flurbiprofen-Loaded Solid SNEDDS Preconcentrate for the Enhanced Solubility, In-Vitro Dissolution and Bioavailability in Rats

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 247 ◽  
Author(s):  
Rae Kim ◽  
Dong-Jin Jang ◽  
Yu Kim ◽  
Jin-Ha Yoon ◽  
Kyoung Min ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Particle Size ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
In Vitro Dissolution ◽  
Enhanced Solubility

The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phase diagram. The pseudo-ternary phase diagram, composed of FL as the drug and dispersion core, Kollisolv MCT 70 as the oil phase, and TPGS (tocopherol polyethylene glycol 1000 succinate) as the surfactant, was constructed for the determination of the SSP region. SSP was investigated in terms of particle size, physical state by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), in vitro dissolution and oral pharmacokinetics in rats. The determined SSP (FL/Kollisolv MCT 70/TPGS = 10/10/80, weight %) in the pseudo-ternary phase diagram had the melting point of 32.37 °C and uniform mean particle size of below 30 nm without any precipitation of FL in the dispersion. In the dissolution test, the SSP exhibited 95.70 ± 3.40% of release at 15 min, whereas the raw FL showed poor dissolution (i.e., 6.75 ± 1.30%) at that time point. In addition, the SSP showed the enhanced oral absorption (i.e., 1.93-fold increase in AUCinfinite) as compared to the suspension group of raw FL. Therefore, the developed SSP would be a promising drug delivery system with excellent solubilization, dissolution, and bioavailability for FL.

Formulation and Optimization of Self Emulsifying Drug Delivery System For Effective Anthelmintic Therapy

2021 ◽  
pp. 5831-5837
Author(s):  
Kiran C. Mahajan ◽  
Smita S. Pimple ◽  
Hemant A. Deokule
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase ◽  
In Vitro Dissolution ◽  
Ternary Phase Diagrams ◽  
Globule Size ◽  
Capmul Mcm ◽  
Negative Zeta Potential

The present study aims to develop and optimize a self-emulsifying drug delivery system for paediatric patients to improve the oral bioavailability of the anthelmintic drug, Praziquantel (PZQ) and to perform it’s in-vitro dissolution study. The solubility of PZQ was estimated in various vehicles to select proper component combination. Capmul MCM (oil), Cremophore RH40 (surfactant) and PEG400 (co-surfactant) were employed to construct pseudo-ternary phase diagrams. Eight formulations composed of Capmul MCM, at Smix ratios (1:1, 2:1 & 3:1) were selected. The optimized formulation F7 has a mean globule size 14.73 nm with a negative zeta potential -44.43 mV. The results indicated that PZQ loaded SEDDS, showed enhanced solubilization and nanosizing potential to improve the absorption of the drug.

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 Quality-By-Design-Based Development of a Voxelotor Self-Nanoemulsifying Drug-Delivery System with Improved Biopharmaceutical Attributes

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1388
Author(s):  
Aristote B. Buya ◽  
Romano Terrasi ◽  
Jérémie K. Mbinze ◽  
Giulio G. Muccioli ◽  
Ana Beloqui ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Ternary Phase Diagram ◽  
Desirability Function ◽  
Limiting Factors ◽  
In Vitro Dissolution

Low aqueous solubility and poor oral bioavailability are limiting factors in the oral delivery of voxelotor, an antisickling agent. To overcome these limitations, a voxelotor self-nanoemulsifying drug delivery system was developed. Various oils, surfactants, and cosurfactants were screened for their solubilization potential for the drug. The area of nanoemulsification was identified using a ternary phase diagram. An experimental mixture design and a desirability function were applied to select SNEDDSs that contain a maximum amount of lipids and a minimum amount of surfactant, and that possess optimal emulsification properties (i.e., droplet sizes, polydispersity index (PDI), emulsification time, and transmittance percentage). The optimized SNEDDS formulation was evaluated for the self-emulsifying time (32 s), droplet size (35 nm), and zeta potential (−8 mV). In vitro dissolution studies indicated a 3.1-fold improvement in drug solubility from the optimized SNEDDS over pure drug powder. After 60 min of in vitro lipolysis, 88% of the voxelotor loaded in the SNEDDS remained in the aqueous phase. Cytotoxicity evaluation, using Caco-2 cells, indicated the safety of the formulation at 0.9 mg/mL. The transport of the voxelotor SNEDDS across Caco-2 monolayers was significantly enhanced compared to that of the free drug. Compared to the drug suspension, the developed SNEDDS enhanced the oral bioavailability (1.7-fold) of voxelotor in rats. The results suggest that further development of SNEDDSs for the oral delivery of voxelotor is needed.

scholarly journals DESIGN AND EVALUATION OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEMS OF MANIDIPINE FOR ENHANCEMENT OF SOLUBILITY

2019 ◽  
pp. 288-295
Author(s):  
SRIKANTH REDDY S ◽  
SURESH G
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Ternary Phase Diagram ◽  
Spherical Shape ◽  
In Vitro Dissolution ◽  
Stability Studies ◽  
Enhanced Solubility ◽  
The Stability

Objective: The present work is aimed at developing liquid self-nanoemulsifying drug delivery system (liquid-SNEDDS) of manidipine. Methods: The manidipine SNEDDS is formulated with excipients comprising Capmul MCM as oil phase, Transcutol P as surfactant, and Lutrol L 300 as cosurfactant. The prepared fifteen formulations of manidipine SNEDDS were performed for emulsification time, percentage transmittance, particle size, drug release, in vitro dissolution and stability studies. Ternary phase diagram plotted using Chemix software. Results: The optimized manidipine liquid SNEDDS formulation (F14) subjected to drug-excipient compatibility studies by Fourier-transform infrared spectroscopy and characterized for particle size, zeta potential, scanning electron microscopy, and stability studies. The morphology of manidipine SNEDDS indicates spherical shape with uniform particle distribution. The percentage drug release from optimized formulation F14 (98.24±5.14%) was higher than that of pure drug (39.17±2.98%). The stability data indicated no noticeable change in drug content, emulsifying properties, drug release, and appearance. Conclusion: Hence, a potential SNEDDS formulation of manidipine developed with enhanced solubility, dissolution rate, and bioavailability.

scholarly journals PREPARATION, CHARACTERIZATION AND STABILITY STUDIES OF SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM OF NIFEDIPINE

2020 ◽  
pp. 94-102
Author(s):  
SABITRI BINDHANI ◽  
SNEHAMAYEE MOHAPATRA ◽  
RAJAT KUMAR KAR
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Linseed Oil ◽  
Stability Study ◽  
In Vitro Dissolution

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 selected for further studies into DSC, SEM, FTIR, and XRD analysis. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM study, it was observed that the drug has been uniformly distributed and having a smooth surface. From the in vitro dissolution study, it improved the dissolution rate of nifedipine which was 98.70% of drug release where pure drug release only 6.72%. Conclusion: In conclusion, a solid self-micro emulsifying drug delivery system is improved the solubility and drug release rate but also improved the stability of the formulation.

scholarly journals Formulation and Characterization of Piroxicam as Self-Nano Emulsifying Drug Delivery System

2020 ◽  
Vol 29 (1) ◽  
pp. 174-183
Author(s):  
Fahad F. Salim ◽  
Nawal A. Rajab
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Stability Study ◽  
Drug Dissolution ◽  
Inflammatory Conditions ◽  
Ternary Phase Diagrams

Piroxicam (PIR) is a nonsteroidal anti-inflammatory drug of oxicam category, used in gout, arthritis, as well as other inflammatory conditions (topically and orally). PIR is practically insoluble in water, therefore the aim is prepare and evaluate piroxicam as liquid self-nanoemulsifying drug delivery system to enhance its dispersibility and stability. The Dispersibilty and Stability study have been conducted in Oil, Surfactant and Co-surfactant for choosing the best materials to dissolve piroxicam. The pseudo ternary phase diagrams have been set at 1:1, 2:1, 3:1 as well as 4:1 ratio of surfactants and co-surfactants, also there are 4 formulations were prepared by using various concentrations of transcutol HP, cremophore EL and triacetin oil. All the constructed prepared formulas have been assessed for in vitro drug dissolution, thermodynamic stability, polydispersity index, robustness to dilution, particle size distribution, drug content, and the dispersibility and emulsification time.From the presented research concluded that the self-nanoemulsifying drug delivery system is the convenient method for improving Dispersibilty and Stability of piroxicam.  Keywords: Pseudo-ternary phase diagram, Dissolution rate, SNEDDS, Piroxicam.

Formulation and Evaluation of Self Nanoemulsifying Drug Delivery System of Nifedipine

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Dinesh Kaushik ◽  
Jyoti Malik ◽  
Satish Sardana ◽  
Chisa Matsubara
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Drug Bioavailability ◽  
Wide Range

Oral route is the most preferred route of drug administration due to its easy accessibility, intake, and wide range of choices making it economical. Currently, greater than 60% of marketed drugs are oral products. Over 90% of therapeutic compounds given orally areknown to possess oral bioavailability limitations. Therefore, there is a need to explore various approaches that can be used to improve oral drug bioavailability besides using physical and chemical means. The objective of this study is to prepare a formulation i.e. self microemulsifying drug delivery system (SMEDDS) of nifedipine with the intention to improve the increase dissolution rate (solubility). This will ensure the quick absorption and uniform bioavailability of nifedipine. Selection of oils, surfactants and co-surfactants was done by determining % transparency and on the basis of compatibility studies by FTIR spectra analysis. Different SMEDDS formulation were prepared of different ratio of oil:surfactantmix (1:9,2:8,3:7,4:6,5:5,6:4,7:3,8:2,9:1) and different ratio of surfactants : cosurfactants. Pseudo ternary phase diagram were constructed by water titration method to obtain a particle micro-emulsion region (on the basis of clarity and transparency). The formulation B-I was optimized because of maximum transparency (87.35%) and maximum % drug entrapment (95.32%). The average droplet size and zeta potential was found 86.05 and -0.189. The solubility of nifedipine increase in SMEDDS formulation upto72.17%.From in vitro dissolution study it was proved that SMEDDS formulation releases drug at faster rate, thus the objective of increase solubility and hence the better dissolution rate for uniform bioavailability via SMEDDS formulation of nifedipine was successfully achieved.

Enhanced Solubility, In-Vitro Dissolution and Lipase Inhibition of a Self-Nanoemulsifying Drug Delivery System Containing Orlistat

2019 ◽  
Vol 19 (2) ◽  
pp. 634-639 ◽  
Author(s):  
Dae Hun Kim ◽  
Pooja Maharjan ◽  
Jae Yeol Kim ◽  
Dong-Jin Jang ◽  
Tae-Sung Koo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Dissolution ◽  
Enhanced Solubility ◽  
Lipase Inhibition

scholarly journals Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tensile Strength ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 

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.

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