GSH- and pH-responsive drug delivery system constructed by water-soluble pillar[5]arene and lysine derivative for controllable drug release

2015 ◽  
Vol 51 (31) ◽  
pp. 6832-6835 ◽  
Author(s):  
Xuan Wu ◽  
Yan Li ◽  
Chen Lin ◽  
Xiao-Yu Hu ◽  
Leyong Wang

GSH- and pH-responsive supramolecular vesicles constructed by a host–guest inclusion complex formed from water-soluble pillar[5]arene and lysine derivative were successfully developed.

Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari

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.


2015 ◽  
Vol 3 (37) ◽  
pp. 7401-7407 ◽  
Author(s):  
Haibo Wang ◽  
Gongyan Liu ◽  
Shihua Dong ◽  
Junjie Xiong ◽  
Zongliang Du ◽  
...  

A multifunctional drug delivery system with AIE character was designed and constructed for simultaneous cellular imaging and pH-triggered drug release.


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.


2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Yan Liu ◽  
Chunling Xie ◽  
Fengfen Zhang ◽  
Xiufeng Xiao

Nanostructured materials play a fundamental role in orthopedic research owing to their outstanding properties and excellent biocompatibility. Titania nanotube (TNT) arrays engineered by electrochemical anodization process have been extensively explored and used as effective carriers for controlled drug delivery. In this study, we proposed a drug delivery system based on coordination bond. Iron (III), Fe3+, on the nanotube surface can effectively bind to alendronate sodium (NaAL), a drug for the treatment of osteoporosis, through coordination bonds, which can be formed or broken through the change of pH, and thus can be controlled by pH. The pH-responsive system was prepared by three-step procedure: (i) fabrication of TNTs by electrochemical anodization, (ii) modification of amino groups on the surface of nanotubes by hydrothermal method, and (iii) amino-functionalized nanotubes by Fe3+ solution soak. The Fe-modified TNTs not only allowed alendronate-loading content of up to 50.2% by weight, which is significantly higher than most drug delivery systems previously reported, but also delayed and prolonged drug release. Moreover, in vitro drug release experiments demonstrated that coordination bond-based TNT system may have great potential applications in clinical use.


2014 ◽  
Vol 2 (33) ◽  
pp. 5409-5418 ◽  
Author(s):  
Bo Yu ◽  
Xiaoling Li ◽  
Wenjie Zheng ◽  
Yanxian Feng ◽  
Yum-Shing Wong ◽  
...  

A cancer-targeted and structure-transformable drug delivery system has been constructed, which displays enhanced anticancer efficacy and exhibits the characteristics of shape transformation and pH-controlled drug release under acidifying cell organelles.


Author(s):  
Sreenivas Patro Sisinthy ◽  
Nalamolu Koteswara Rao ◽  
Chin Yi Lynn Sarah

<p><strong>Objective: </strong>The objective of the present study was to design, optimise and characterise self nano emulsifying drug delivery systems (SNEDDS) for a poorly water soluble drug, olmesartan medoxomil (OLM) by Formulation by Design (FbD) approach with an aim to improve its solubility and dissolution.</p><p><strong>Methods: </strong>The SNEDDS were systematically optimised using three factor Box-Behnken design. Concentration of formulation variables, namely, the oil phaseX1 (Capryol 90), the surfactant X2 (Cremophor EL), and the co-surfactant X3 (Transcutol P), was optimized for its impact on mean globule size (Y1), percentage drug release in 20 min (Y2) and turbidity (Y3) of the formulation. Ternary phase diagrams were constructed to select the areas of nanoemulsion and the amounts of oil, surfactant and cosurfactants as critical formulation variables. The prepared SNEDDS were characterised for globule size, dissolution studies, turbidity, and transmission electron microscopy (TEM).</p><p><strong>Results: </strong>Following optimisation, the values of formulation variables were found to be 142.276 mg (Capryol P), 399.999 mg (Cremophor EL) and 598.871 mg (Transcutol P) which produced a globule size of 12.64 nm, percentage drug release of 93.34% and a turbidity of 0.02 FNU. TEM studies demonstrated spherical droplet morphology.</p><p><strong>Conclusion: </strong>Thus, the present studies reveal that the SNEDDS is a promising drug delivery system approach for the enhancement of solubility and dissolution rate of OLM.</p>


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