scholarly journals In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility

2021 ◽  
Vol 14 (11) ◽  
pp. 1089
Author(s):  
Hakan Nazlı ◽  
Burcu Mesut ◽  
Yıldız Özsoy
Keyword(s):  
Drug Delivery ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Ternary Phase Diagrams ◽  
Enhanced Solubility ◽  
Porous Carriers ◽  
Drug Precipitation ◽  
Precipitation Inhibitors ◽  
Preformulation Studies

Aprepitant (APR) belongs to Class II of the Biopharmaceutical Classification System (BCS) because of its low aqueous solubility. The objective of the current work is to develop self-nanoemulsifying drug delivery systems (SNEDDS) of APR to enhance its aqueous solubility. Preformulation studies involving screening of excipients for solubility and emulsification efficiency were carried out. Pseudo ternary phase diagrams were constructed with blends of oil (Imwitor® 988), cosolvent (Transcutol® P), and various surfactants (Kolliphor® RH40, Kolliphor® ELP, Kolliphor® HS15). The prepared SNEDDS were characterized for droplet size and nanoemulsion stability after dilution. Supersaturated SNEDDS (super-SNEDDS) were prepared to increase the quantity of loaded APR into the formulations. HPMC, PVP, PVP/VA, and Soluplus® were used as polymeric precipitation inhibitors (PPI). PPIs were added to the formulations at 5% and 10% by weight. The influence of the PPIs on drug precipitation was investigated. In vitro lipolysis test was carried out to simulate digestion of formulations in the gastrointestinal tract. Optimized super-SNEDDS were formulated into free-flowing granules by adsorption on the porous carriers such as Neusilin® US2. In vitro dissolution studies of solid super-SNEDDS formulation revealed an increased dissolution rate of the drug due to enhanced solubility. Consequently, a formulation to improve the solubility and potentially bioavailability of the drug was developed.

Design, Optimization and Evaluation of Repaglinide Self-Nanoemulsifying Drug Delivery for Enhanced Solubility

2017 ◽  
Vol 10 (6) ◽  
pp. 3920-3928
Author(s):  
Mahalaxmi K ◽  
Sailu Ch
Keyword(s):  
Drug Delivery ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Antidiabetic Drug ◽  
Water Soluble Drug ◽  
Enhanced Solubility ◽  
Poorly Water Soluble ◽  
Capmul Mcm ◽  
Poorly Water Soluble Drug

The aim of study was to develop self-nanoemulsifying systems of poorly water-soluble drug repaglinide, which is an antidiabetic drug in the class of medications known as meglitinides. Solubility of repaglinide in oily phases and surfactants was determined to identify components of self-nanoemulsifying drug delivery system (SNEDDS). Surfactants and oil was selected based on solubility studies were further screened for their efficiency in formulation. Acrysol K 150, Kolliphor EL and Capmul MCM were selected as oil, surfactant and co-surfactant respectively. Formulation F8 was found to be optimized formulation on the basis of in vitro dissolution studies, particle size and zeta potential. The optimized formulation was then subjected to stability studies and was found to be stable after 6 months. Thus, SNEDDS were found to be influential in improving the release performance of repaglinide, indicating their potential to improve the solubility and oral bioavailability of repaglinide.  

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.

In-Vitro and In-Vivo Evaluation of Supersaturable Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Dutasteride

2020 ◽  
Vol 17 (1) ◽  
pp. 74-86 ◽  
Author(s):  
Poonguzhali Subramanian ◽  
P. S. Rajnikanth ◽  
Manish Kumar ◽  
Kumarappan Chidambram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Absorption ◽  
Drug Loading ◽  
Methyl Cellulose ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Drug Load

Objective: A novel, Supersaturable Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) has been prepared to improve the Dutasteride's poor aqueous solubility. Methods: By adding Hydroxy Propyl Methyl Cellulose (HPMC) as a precipitation inhibitor to conventional SNEDDS, a supersaturable system was prepared. Firstly, the prepared SNEDDS played an important role in increasing the aqueous solubility and hence oral absorption due to nano-range size. Secondly, the S-SNEDDS found to be advantageous over SNEDDS for having a higher drug load and inhibition of dilution precipitation of Dutasteride. Formulated S-SNEDDS (F1-F9) ranged from 37.42 ± 1.02 to 68.92 ± 0.09 nm with PDI 0.219-0.34 and drug loading of over 95 percent. Results: The study of in-vitro dissolution revealed higher dissolution for S-SNEDDS compared to SNEDDS and Avodart soft gelatin capsule as a commercial product. In addition, higher absorption was observed for S-SNEDDS showing approximately 1.28 and 1.27 fold AUC (0-24h) and Cmax compared to commercial products. Therefore, S-SNEDDS has proven as a novel drug delivery system with a higher drug load, higher self-emulsification efficiency, higher stability, higher dissolution and pronounced absorption. Conclusion: In conclusion, S-SNEDDS could be a new emerging approach to enhance aqueous solubility in many folds for drugs belonging to BCS Class II and IV and thus absorption and oral bioavailability.

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 FORMULATION AND EVALUATION OF SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF GLICLAZIDE

2016 ◽  
Vol 8 (11) ◽  
pp. 144
Author(s):  
Suwarna R. Deshmukh ◽  
Suparna S. Bakhle ◽  
Kanchan P. Upadhye ◽  
Gouri R. Dixit
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Water Soluble Drug

Objective: Gliclazide (GCZ) is a widely prescribed anti-diabetic drug belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. The present investigations highlight the development of solid self-emulsifying drug delivery system (solid-SEDDS) for improved oral delivery of the poorly water-soluble drug, GCZ.Methods: Various oils, surfactant and co-surfactant, were screened for their emulsification ability. Ternary phase diagrams were plotted to identify the zone of micro-emulsification. Liquid SEDDS of the drug were formulated using lemon oil as the oil phase, tween 80, as the surfactant, and labrasol, as the co-surfactant. The optimized liquid SEDDS was transformed into free-flowing powder using florite R as the adsorbent. Results: Self-emulsifying powder retained the self-emulsifying property of the liquid SEDDS. The morphology of solid-SEDDS from scanning electron microscopy studies demonstrated the presence of spherical, granular particles indicating good flowing ability. X-ray powder diffraction studies confirmed solubilization of the drug in the lipid excipients and/or transformation of a crystalline form of the drug to amorphous form. In vitro dissolution studies revealed enhanced release of the drug from solid-SEDDS as compared to plain drug and marketed formulation.Conclusion: Thus it can be concluded that solid-SEDDS, amenable for the development of solid dosage form, can be successfully developed using florite R with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug.

scholarly journals Effect of inclusion of citric acid and Lutrol® F-68 on ziprasidone and β-cyclodextrin complexation: Characterization, solubility and dissolution studies

2020 ◽  
Vol 11 (4) ◽  
pp. 280-284
Author(s):  
Vaishali Yogesh Londhe ◽  
Sreevidya Ramesh Krishnan
Keyword(s):  
Citric Acid ◽  
Antipsychotic Agent ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Solubility Study ◽  
Dissolution Studies ◽  
Enhanced Solubility ◽  
Ft Ir

Ziprasidone (ZPR) is an antipsychotic agent having less solubility. It is used for the treatment of schizophrenia. Complexation of hydrophobic drugs with cyclodextrins leads to enhanced solubility and dissolution. In this study, inclusion complexes were prepared by different methods, using ZPR, β-cyclodextrin (β-CD), and different auxiliary agents like hydrophilic polymer and hydroxy acid (1:1:0.5) to improve the aqueous solubility. The characterization of the ternary complexes was carried out using solubility study, Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Fourier transformation infrared spectroscopy (FT-IR) and in vitro dissolution studies. DSC, XRD, and FT-IR studies showed interaction in drug, cyclodextrin, and auxiliary agents which are confirmed by enhancement of solubility and dissolution. Spray-dried dispersion showed less crystallinity and higher solubility as compared to the kneading method for both citric acid and Lutrol® F-68. Thus, the investigation concludes that the presence of the auxiliary agent has a synergistic action on complexation with cyclodextrin, which helps to modify the physicochemical properties of the drug.

PCL-based nanofibers containing ibuprofen/cyclodextrins nanocontainers: A potential candidate for drug delivery application

2018 ◽  
Vol 48 (9) ◽  
pp. 1420-1438 ◽  
Author(s):  
Saeideh Masoumi ◽  
Sahar Amiri ◽  
Seyed Hajir Bahrami
Keyword(s):  
Drug Delivery ◽  
Inclusion Complex ◽  
Aqueous Solubility ◽  
Microscopy Study ◽  
Electron Microscopy Study ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Potential Candidate ◽  
Scanning Calorimetry

Poor solubility and low dissolution rate of ibuprofen (IBU) in the aqueous gastro-intestinal fluids restrict its application, absorption, distribution, target organ delivery, and bioavailability. For improvement of aqueous solubility of IBU, supramolecular nanocontainers of IBU/cyclodextrin were prepared via formation of inclusion complex between ibuprofen and cyclodextrins (α-cyclodextrin and β-cyclodextrin) at various conditions (at room temperature at 25℃ and under sonic energy). The formation of inclusion complex between IBU and cyclodextrins can be confirmed by hydrogen nuclear magnetic resonance, differential scanning calorimetry, fourier transform Infrared spectroscopy (FTIR), X-ray diffraction, and scanning electron microscopy study. FTIR of pure IBU and cyclodextrins is similar to the obtained complex, which indicated intactness of drug in the complex. The encapsulation of IBU in cyclodextrins cavity improved its solubility, phase solubility, and in vitro dissolution and also controlled its release which ensures the long-term delivery. Electro-spun nanofibers of poly-ɛ-caprolactone containing IBU/cyclodextrins is a promising method for controlled drug delivery electro-spun which is bead-free without any aggregation on the surface.

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.

Development and characterization of ternary system for solubility enhancement of a second-generation COX-II inhibitor

2016 ◽  
Vol 5 (12) ◽  
pp. 5163
Author(s):  
Santosh Girani* ◽  
Shidallingapa Zalki ◽  
Mahantesh Kavatekar ◽  
Ajay Shahapur ◽  
Vitthal K. Vijapure
Keyword(s):  
Ternary Systems ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Complexing Agents ◽  
High Permeability ◽  
Bcs Class Ii ◽  
Enhanced Solubility

Etoricoxib is a highly selective COX-II inhibitor, used to treat pains of different etiologies. Etoricoxib has low aqueous solubility (201g/ml) and high permeability and therefore classified as BCS class II drug. By formulating these drugs with cyclodextrins as inclusion complexes have shown to increase the bioavailability. Cyclodextrins when used as complexing agents, enhance the solubility of poor water soluble lipophilic drugs. The objective of the present work is to formulate Etoricoxibcyclodextrin complexes by using ternary systems as Citric acid, Tartaric acid and PVP K-30 in order to enhance solubility and evaluate the enhanced solubility by in-vitro dissolution.

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
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