Olmesartan Medoxomil-Loaded Self-Nanoemulsifying Drug Delivery Systems: Design, In-Vitro Characterization, and Pharmacokinetic Assessments in Rabbits Via LC-MS/MS

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
El-Assal M. I. A. ◽  
El-Gendy M. A. ◽  
Tadros M. I. ◽  
El-Gazayerly O. N.
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Drug Delivery Systems ◽  
Oral Absorption ◽  
Systems Design ◽  
Olmesartan Medoxomil ◽  
Delivery Systems ◽  
Log P ◽  
Polyethylene Glycol 400

Olmesartan medoxomil (OLM) is a lipophilic (log P = 4.31) antihypertensive drug suffering from limited oral bioavailability in humans (26%) due to its low aqueous solubility, uncontrolled enzymatic conversion to the active metabolite (olmesartan; OL) and efflux by drug resistance pumps. Surmounting such limitations via incorporation of OLM into self-nanoemulsifying drug delivery systems (SNEDDS). Based on OLM-equilibrium solubility studies in various oils, surfactants and co-surfactants, Capmul® MCM, Tween® 20, Cremophor® EL and polyethylene glycol-400 (PEG) were combined in different ratios to plot ternary phase diagrams. OLM-loaded SENDDS were developed and evaluated for particle size, polydispersity index (PDI), zeta potential, self-emulsification time, morphology, drug released percentages after 5-min (Q5min%), 1-hour (Q1h%) and dissolution efficiency percentages (DE1h%). The OL pharmacokinetics from SNEDDS (F6) and Benicar® tablets were evaluated (LC-MS/MS) in rabbits. Spherical OLM-loaded SNEDDS were developed. The best-achieved SNEDDS (F6) showed short emulsification time (13 s), fine droplet size (60.00 nm), low PDI (0.25), negative zeta potential (-14.4 mV), promising dissolution parameters; Q5min% (29.78%), Q1h% (66.69%) and DE1h%(47.96%) and enhanced in vivo absorption characteristics; shorter Tmax, higher Cmax and larger AUC(0−48h; suggesting its potential for the enhancement of the oral absorption of practically insoluble drugs; like OLM.

scholarly journals Predicting Oral Absorption of fenofibrate in Lipid-Based Drug Delivery Systems by Combining In Vitro Lipolysis with the Mucus-PVPA Permeability Model

2021 ◽  
Vol 110 (1) ◽  
pp. 208-216
Author(s):  
Margherita Falavigna ◽  
Mette Klitgaard ◽  
Ragna Berthelsen ◽  
Anette Müllertz ◽  
Gøril Eide Flaten
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Absorption ◽  
Delivery Systems ◽  
Permeability Model ◽  
In Vitro Lipolysis

Using in vitro lipolysis and SPECT/CT in vivo imaging to understand oral absorption of fenofibrate from lipid-based drug delivery systems

2020 ◽  
Vol 317 ◽  
pp. 375-384 ◽  
Author(s):  
Thuy Tran ◽  
Peter Bønløkke ◽  
Cristina Rodríguez-Rodríguez ◽  
Zeynab Nosrati ◽  
Pedro Luis Esquinas ◽  
...  
Keyword(s):  
Drug Delivery ◽  
In Vivo Imaging ◽  
Drug Delivery Systems ◽  
Oral Absorption ◽  
Delivery Systems ◽  
In Vitro Lipolysis

Development and in vitro evaluation of zeta potential changing self-emulsifying drug delivery systems for enhanced mucus permeation

2016 ◽  
Vol 510 (1) ◽  
pp. 255-262 ◽  
Author(s):  
Wongsakorn Suchaoin ◽  
Irene Pereira de Sousa ◽  
Kesinee Netsomboon ◽  
Hung Thanh Lam ◽  
Flavia Laffleur ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
In Vitro Evaluation

scholarly journals FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF DRUG DELIVERY SYSTEMS BASED TELMISARTAN ENCAPSULATED IN SILK FIBROIN NANOSPHERE’S

2019 ◽  
Vol 11 (1) ◽  
pp. 247 ◽  
Author(s):  
Shahid Ud Din Wani ◽  
Gangadharappa H. V. ◽  
Ashish N. P.
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Zeta Potential ◽  
Silk Fibroin ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Random Coil ◽  
Burst Release

Objective: The aim of the present work was to formulate silk fibroin (SF) nanospheres (NS’s) for drug delivery application. The current study was designed to advance the water solubility and bio-availability of telmisartan by nanoprecipitation method.Methods: SF NS’s loaded with TS were prepared by nanoprecipitation method. The drug was dissolved in aqueous solution of SF by using acetone as a non-solvent. The prepared NS’s were then characterized by FTIR, X-ray diffraction and zeta potential, and were evaluated for its, surface morphology, %drug content, encapsulation efficiency and in vitro drug release.Results: The evaluation results of SF NS’s loaded of TS showed 74.22±0.17 % entrapment efficiency, 35.21±0.02 % of drug loading, and-4.9 mV to-13.6 mV of zeta potential due to the proper bounding of TS with the β-sheets of SF, the particle size reported was within the size range of 160-186 nm having smooth surface and were spherical in shape. The SFNS’s pattern switched from random coil to β-sheet formation on treating with acetone. FTIR and DSC studies marked no such inter-molecular interactions between SF and drug molecules. The % cumulative in vitro drug release from SF NS’s exhibited quick burst release. The in vitro cumulative drug release of SF NS’s of TS it was found that about 74% of the drug was released within 8 h and about 96% of drug released at 24 hr. The rate of drug release increased with the increase in SF ratio.Conclusion: It is believed that these SF NS’s will find potential applications in drug delivery release as drug carriers, especially poor water-soluble drugs. All these results proposed that SF NS’s are eventuality handy in various drug delivery systems.

scholarly journals Linagliptin loaded Solid-SMEEDS for enhanced solubility and dissolution: Formulation development and optimization by D-optimal design

2019 ◽  
Vol 9 (2) ◽  
pp. 47-56
Author(s):  
Madhubhai M Patel ◽  
Rahulkumar J Patel
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Transmission Electron Microscopy ◽  
Optimal Design ◽  
Zeta Potential ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Dissolution Profile ◽  
Transmission Electron

The aim of the present investigation was to formulate and evaluate solid self-micro emulsifying drug-delivery systems (S-SMEDDS) to improve solubility and dissolution profile of Linagliptin. Solubility of Linagliptin in different oils, surfactants and co-surfactants was assessed and optimizations of pseudo-ternary plots were also carried out for preparation of liquid SMEDDS. D-optimal design mixture was used in the optimization of Linagliptin loaded liquid SMEEDS. The optimized SMEEDS were characterized for globule size, zeta potential, dilution stability, transmittance, pH and in-vitro release profile. The morphology of the Linagliptin SMEEDS was observed by Transmission Electron Microscopy (TEM). Among the different silicates, Nusillin US2 was used as the solid carrier/absorbent to formulate S-SMEEDS of Linagliptin. Improved in-vitro dissolution profile of optimized formulation was observed, resulting in multifold improvement in the absorption profile of Linagliptin as compared with pure drug. In a nutshell, this optimized S-SMEDD formulation holds great promise for enhancement of its physiochemical and biological attributes. Keywords: Linagliptin, Solid Self-micro Emulsifying Drug Delivery Systems, D-optimal design, Zeta-potential, Transmission Electron Microscopy

Lipid Nanocarriers for Oral Delivery of Serenoa repens CO2 Extract: A Study of Microemulsion and Self-Microemulsifying Drug Delivery Systems

Planta Medica ◽  
2018 ◽  
Vol 84 (09/10) ◽  
pp. 736-742 ◽  
Author(s):  
Clizia Guccione ◽  
Maria Bergonzi ◽  
Khaled Awada ◽  
Vieri Piazzini ◽  
Anna Bilia
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Oral Absorption ◽  
Delivery Systems ◽  
Array Detector ◽  
Serenoa Repens ◽  
Lipid Nanocarriers

AbstractThe aim of this study was the development and characterization of lipid nanocarriers using food grade components for oral delivery of Serenoa repens CO2 extract, namely microemulsions (MEs) and self-microemulsifying drug delivery systems (SMEDDSs) to improve the oral absorption. A commercial blend (CB) containing 320 of S. repens CO2 extract plus the aqueous soluble extracts of nettle root and pineapple stem was formulated in two MEs and two SMEDDSs. The optimized ME loaded with the CB (CBM2) had a very low content of water (only 17.3%). The drug delivery systems were characterized by dynamic light scattering, transmission electron microscopy, and high-performance liquid chromatography (HPLC) with a diode-array detector analyses in order to evaluate the size, the homogeneity, the morphology, and the encapsulation efficiency. β-carotene was selected as marker for the quantitative HPLC analysis. Additionally, physical and chemical stabilities were acceptable during 3 wk at 4 °C. Stability of these nanocarriers in simulated stomach and intestinal conditions was proved. Finally, the improvement of oral absorption of S. repens was studied in vitro using parallel artificial membrane permeability assay. An enhancement of oral permeation was found in both CBM2 and CBS2 nanoformulations comparing with the CB and S. repens CO2 extract. The best performance was obtained by the CBM2 nanoformulation (~ 17%) predicting a 30 – 70% passive oral human absorption in vivo.

scholarly journals Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 489
Author(s):  
Mette Klitgaard ◽  
Anette Müllertz ◽  
Ragna Berthelsen
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Absorption ◽  
Aqueous Suspension ◽  
Delivery Systems ◽  
Time Curve ◽  
Drug Permeation ◽  
In Vitro Lipolysis

The aim of this study was to design an in vitro lipolysis-permeation method to estimate drug absorption following the oral administration of self-nanoemulsifying drug delivery systems (SNEDDSs). The method was evaluated by testing five oral formulations containing cinnarizine (four SNEDDSs and one aqueous suspension) from a previously published pharmacokinetic study in rats. In that study, the pharmacokinetic profiles of the five formulations did not correlate with the drug solubilization profiles obtained during in vitro intestinal lipolysis. Using the designed lipolysis-permeation method, in vitro lipolysis of the five formulations was followed by in vitro drug permeation in Franz diffusion cells equipped with PermeaPad® barriers. A linear in vivo–in vitro correlation was obtained when comparing the area under the in vitro drug permeation–time curve (AUC0–3h), to the AUC0–3h of the plasma concentration–time profile obtained from the in vivo study. Based on these results, the evaluated lipolysis-permeation method was found to be a promising tool for estimating the in vivo performance of SNEDDSs, but more studies are needed to evaluate the method further.

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