scholarly journals Cubosomes with surface cross-linked chitosan exhibit sustained release and bioavailability enhancement for vinpocetine

RSC Advances ◽  
2019 ◽  
Vol 9 (11) ◽  
pp. 6287-6298 ◽  
Author(s):  
Yuanfeng Wei ◽  
Jianjun Zhang ◽  
Yazhen Zheng ◽  
Yaxiang Gong ◽  
Meng Fu ◽  
...  

Cubosomes with surface cross-linked chitosan exhibit anti-digestion effect, sustained drug release behavior, and significantly enhanced oral bioavailability of vinpocetine.

Author(s):  
Kumara Swamy S ◽  
Ramesh Alli

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.


2018 ◽  
Vol 6 (7) ◽  
pp. 1035-1043 ◽  
Author(s):  
Jian He ◽  
Lisha Ai ◽  
Xin Liu ◽  
Hao Huang ◽  
Yuebin Li ◽  
...  

The NIR-laser-driven plasmonic photothermal and sustained drug release behavior of CuS–PTX/SiO2 nanocapsules show great synergistic chemo-photothermal therapeutic effects on cancer cells in vitro and in vivo.


2018 ◽  
Vol 12 (6) ◽  
pp. 822-826
Author(s):  
Lei Jiang ◽  
Chen Su ◽  
Zhongjie Zhu ◽  
Yanyi Wen ◽  
Shan Ye ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1717
Author(s):  
Lei Xu ◽  
Qingliang Yang ◽  
Wei Qiang ◽  
Huijie Li ◽  
Weizhen Zhong ◽  
...  

Three-dimensional (3D) printing technology, specifically stereolithography (SLA) technology, has recently created exciting possibilities for the design and fabrication of sophisticated dosages for oral administration, paving a practical way to precisely manufacture customized pharmaceutical dosages with both personalized properties and sustained drug release behavior. However, the sustained drug release achieved in prior studies largely relies on the presence of hydrophilic excipients in the printing formulation, which unfortunately impedes the printability and formability of the corresponding printing formulations. The current study developed and prepared mini-sized oral pellets using the SLA technique and successfully accomplished a hydrophilic excipient-independent drug release behavior. With ibuprofen as the model drug, the customized photopolymerizable printing formulation included polyethylene glycol diacrylate (PEGDA) as a monomer and diphenyl (2,4,6-trimethylbenzoyl) phosphine oxide (TPO) as a photoinitiator. The produced mini-sized pellets were thoroughly investigated for various factors, including their printability, physical properties, microscopic features, drug content, and drug-release profiles. The drug release profiles from the printed pellets that were larger size (3 mm and 6 mm) followed the Ritger–Peppas model, demonstrating that the release was influenced by both the diffusion of the dissolved drug and by the erosion of the hydrophilic excipients (PEG400). The profiles from the smaller printed pellets (1 mm and 2 mm) followed first release kinetics, not only illustrating that the release was impacted only by drug diffusion, but also indicating that there is a size boundary between the dependent and independent hydrophilic excipients. These results could create practical benefits to the pharmaceutical industry in terms of the design and development personalized dosages using the SLA printing technique with controllable drug release by manipulating size alone.


RSC Advances ◽  
2020 ◽  
Vol 10 (27) ◽  
pp. 15715-15725 ◽  
Author(s):  
Qi Lian ◽  
Han Liu ◽  
Xuefang Zheng ◽  
Dandan Jia ◽  
Chun Liu ◽  
...  

The schematic preparation of a new kind of pH-sensitive PAN nanoflower and its potential application for UC therapy. PAN (TBP) nanoflowers at pH 7.4 showed good sustained-release (t83% = 260 h), which best fitted the Riger–Peppas model.


Author(s):  
H. C. KIRAN ◽  
DHANDAPANI NAGASAMY VENKATESH ◽  
RAMAN RAJESHKUMAR

Objective: The main aim of the present investigation was to formulate and evaluate microbeads of zaltoprofen. Zaltoprofen, a BCS class II drug used in the treatment of rheumatoid arthritis. Zaltoprofen has a shorter half-life of 2.8 h, and it is administered at a dose of 80 mg thrice a day. By encapsulating the drug into microbeads, it is expected that the release of the drug would be prolonged and thereby, it reduces the frequency of administration and better patient compliance may be improved. Methods: Gellan-chitosan and calcium chloride beads of zaltoprofen were prepared employing ionotropic gelation method using different concentrations of gellan, chitosan, calcium chloride and zaltoprofen. The microbeads were evaluated for its various Physico-chemical parameters such as particle size determination, drug entrapment efficiency, infrared spectroscopy study, differential scanning calorimetry, X-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo oral bioavailability studies. Results: The results suggested that the batch FG-II exhibited higher drug entrapment efficiency (72.42±0.013), a sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an enhanced oral bioavailability (2.4 times higher than that of pure drug), lower elimination rate (1.14 times lesser for the drug in microbeads) with prolonged elimination half-life (2.561 times higher than pure zaltoprofen). Conclusion: Zaltoprofen entrapped microbeads demonstrated as a better delivery system for the sustained release of drug and also to circumvent the drawbacks associated with conventional therapy.


Polymers ◽  
2018 ◽  
Vol 10 (12) ◽  
pp. 1405 ◽  
Author(s):  
Yoshito Wakui ◽  
Takafumi Aizawa

A controlled-release system for drug delivery allows the continuous supply of a drug to the target region at a predetermined rate for a specified period of time. Herein, the sustained release behavior of a drug-containing tablet fabricated through CO2-assisted polymer compression (CAPC) was investigated. CAPC involves placing the drug in the center of a nonwoven fabric, sandwiching this fabric between an integer number of nonwoven fabrics, and applying pressure bonding. An elution test, in which the drug-carrying tablet was immersed in water, showed that sustained-release performance can be controlled by the number of nonwoven fabrics covering the top and bottom of the drug-loaded fabric and compression conditions. A model of sustained drug release was formulated to estimate the effective diffusion coefficient in the porous material. Comparative analysis of the bulk diffusion coefficient revealed that the change in diffusion volume due to change in porosity predominates. The tortuosity of the diffusion path was 3–4, and tended to remain almost constant or increase only slightly when the compression rate was increased. These findings show that sustained drug release can be controlled by incorporating the drug into a nonwoven fabric and using the same raw material to encapsulate it.


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