A novel surface-coated nanocarrier for efficient encapsulation and delivery of camptothecin to cells

MedChemComm ◽  
2014 ◽  
Vol 5 (10) ◽  
pp. 1515-1519 ◽  
Author(s):  
Rie Wakabayashi ◽  
Ryutaro Ishiyama ◽  
Noriho Kamiya ◽  
Masahiro Goto
Keyword(s):  
Anticancer Agent ◽  
Water Soluble ◽  
Poorly Water Soluble

In the present study, we developed a novel surface-coated nanocarrier (SCN) for efficient and stable encapsulation of a poorly water-soluble anticancer agent, camptothecin (CPT).

scholarly journals High loading of trimethylglycine promotes aqueous solubility of poorly water-soluble cisplatin

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Riki Kadokawa ◽  
Tetsuo Fujie ◽  
Gyanendra Sharma ◽  
Kojiro Ishibashi ◽  
Kazuaki Ninomiya ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Anticancer Agent ◽  
Hepatic Arterial Infusion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
High Loading ◽  
High Concentration ◽  
High Solubility ◽  
Arterial Infusion ◽  
Poorly Water Soluble

AbstractTrimethylglycine (TMG) is a cheap, natural, and highly biocompatible compound. Therefore, it has been used in the fields of food and life sciences, but the application of solid TMG is limited to utilisation as an “additive”. In the present study, we focussed on the high solubility of TMG in water, derived from the aprotic zwitterionic structure, and proposed TMG as the chemical accounting for a major portion of the aqueous solution (e.g., 50 wt%). High loading of TMG shifted the properties of water and enabled the dissolution of poorly water-soluble cisplatin, an anticancer agent, at high concentration (solubility of cisplatin: 0.15 wt% in water vs 1.7 wt% in TMG aqueous solution). For hepatic arterial infusion, this can reduce the amount of cisplatin administered from 40 to 4 mL. It enables simple injection using a syringe, without the need for catheters and automatic pumps, leading to critical alleviation of the risk to patients. Furthermore, we produced a dry powder from a cisplatin-containing TMG aqueous solution via freeze-drying. Powders can be conveniently stored and transported. Furthermore, cisplatin is often used as a mixture with other drugs, and cisplatin aqueous solutions are not preferred as they dilute the other drugs.

scholarly journals Slow-targeted release of a ruthenium anticancer agent from vitamin B12 functionalized marine diatom microalgae

2018 ◽  
Vol 47 (48) ◽  
pp. 17221-17232 ◽  
Author(s):  
Joachim Delasoie ◽  
Jérémie Rossier ◽  
Laetitia Haeni ◽  
Barbara Rothen-Rutishauser ◽  
Fabio Zobi
Keyword(s):  
Vitamin B12 ◽  
Cell Lines ◽  
Targeted Delivery ◽  
Anticancer Agent ◽  
Release Profile ◽  
Water Soluble ◽  
Marine Diatom ◽  
Vitamin B ◽  
Poorly Water Soluble ◽  
Targeted Release

Bio-inspired drug capsules: The synthesis of a new vitamin-B12 modified biomaterial with increased static adherence properties toward cancer cell lines, allowed the targeted delivery of a poorly water-soluble ruthenium drug with an unprecedented release profile.

scholarly journals Electrosprayed mesoporous particles for improved aqueous solubility of a poorly water soluble anticancer agent: in vitro and ex vivo evaluation

2018 ◽  
Vol 278 ◽  
pp. 142-155 ◽  
Author(s):  
Elshaimaa Sayed ◽  
Christina Karavasili ◽  
Ketan Ruparelia ◽  
Rita Haj-Ahmad ◽  
Georgia Charalambopoulou ◽  
...  
Keyword(s):  
Anticancer Agent ◽  
Ex Vivo ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Poorly Water Soluble ◽  
Mesoporous Particles

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

scholarly journals Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2591
Author(s):  
Thuan Thi Duong ◽  
Antti Isomäki ◽  
Urve Paaver ◽  
Ivo Laidmäe ◽  
Arvo Tõnisoo ◽  
...  
Keyword(s):  
Thin Film ◽  
Drug Release ◽  
Size Distribution ◽  
Water Soluble ◽  
Release Behavior ◽  
Uniform Size ◽  
Ethanol Injection ◽  
Drug Release Behavior ◽  
Poorly Water Soluble

Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.

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