Predicting Dissolution of Entecavir Using the Noyes Whitney Equation

Kang, Yanlei; Chen, Jiahui; Duan, Zhenyu; Li, Zhong

doi:10.14227/dt300123p38

Cited by 2 publications

(1 citation statement)

References 17 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The results show an average dissolution rate of 5 × 10 –13 ng·s –1 , once again, the dissolution rate is lower than those calculated for the cannabinoid in this study. Similar results have been reported in the last 5 years for drugs, such as itraconazole, entecavir, and cromakalim, diproteverine HC1, and ephedrine with low solubility rates on the order of mg per minute. The described results are explained by considering the virtue of nanosized carriers to increase the solubility of active principles by increasing the solute–solvent interaction at the atomic level, unlike the active principles in tablets.…”

Section: Resultssupporting

confidence: 88%

Nanoliposomes for Controlled Release of Cannabinodiol at Relevant Gastrointestinal Conditions

Zapata,

Rosales,

Rios

et al. 2023

ACS Omega

View full text Add to dashboard Cite

Cannabidiol (CBD) has significant therapeutic potential; nevertheless, its advance as an effective drug by the pharmaceutical business is hindered by its inherent characteristics, such as low bioavailability, low water solubility, and variable pharmacokinetic profiles. This research aimed to develop nanoliposomes using an easy and low-cost method to improve the hydrosolubility of CBD and achieve a controlled delivery of the active principle under relevant physiological conditions from the mouth to the intestine; the cytotoxic and antitumor activities were also evaluated. To achieve the objective, core−shell nanoliposomes based on CBD were synthesized in three easy steps and characterized in terms of shape, size, surface chemistry, thermal capacity, and surface charge density through transmission electron microscopy (TEM), dynamic light scattering (DLS), Fourier transform infrared (FTIR), thermogravimetric analysis (TGA), and potential charge (PZ), respectively. CBD-controlled delivery trials were carried out under simulated mouth−duodenal conditions and fitted to Korsmeyer−Peppas and Noyes−Whitney models to conclude about the pharmacokinetics of CBD from nano-CBD. Cytotoxicity studies on nonmalignant human keratinocytes (HaCaT) were carried out to evaluate its safety and the recommended consumption dose, and finally, the antiproliferative capacity of nano-CBD on human colon carcinoma cells (SW480) was determined as beginning proposal for cancer treatment. The characterization results verified the water solubility for the CBD nanoencapsulated, the core−shell structure, the size in the nanometric regime, and the presence of the synthesis components. The dissolution rate at duodenal conditions was higher than that in buccal and stomach environments, respectively, and this behavior was associated with the shell (lecithin) chemical structure, which destabilizes at pH above 7.2, allowing the release by non-Fickian diffusion of CBD as corroborated by the Korsmeyer−Peppas model. In vitro biological tests revealed the innocuousness and cyto-security of nano-CBD up to 1000 mg•L −1 when evaluated on HaCaT cells and concentrations higher than 1000 mg•L −1 showed antitumor activity against human colon carcinoma cells (SW480) taking the first step as a chemotherapeutic proposal. These results are unprecedented and propose a selective delivery system based on nano-CBD at low cost and that provides a new form of administration and chemo treatment.

show abstract

Section: Resultssupporting

confidence: 88%

Nanoliposomes for Controlled Release of Cannabinodiol at Relevant Gastrointestinal Conditions

Zapata,

Rosales,

Rios

et al. 2023

ACS Omega

View full text Add to dashboard Cite

show abstract

Bioactive Properties and In Vitro Digestive Release of Cannabidiol (CBD) from Tailored Composites Based on Carbon Materials

Zapata,

Vélez,

Correa

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

The use of carriers to improve cannabidiol (CBD) bioavailability during digestion is at the forefront of research. The main objective of this research was to evaluate CBD bioactivity and develop CBD composites based on tailored carbon support to improve availability under digestive conditions. The antioxidant capacity of CBD was evaluated using spectrophotometric methods, and anti-proliferative assays were carried out using human colon carcinoma cells (SW480). Twenty-four composites of CBD + carbon supports were developed, and CBD desorption tests were carried out under simulated digestive conditions. The antioxidant capacity of CBD was comparable to and superior to Butylhydrox-ytoluene (BHT), a commercial antioxidant. CBD reflected an IC-50 of 10,000 mg/L against SW480 cancer cells. CBD in biological systems can increase the shelf life of lipid and protein foods by 7 and 470 days, respectively. Finally, acid carbons showed major CBD adsorption related to electrostatic interactions, but basic carbons showed better delivery properties related to electrostatic repulsion. A tailored composite was achieved with a CBD load of 27 mg/g with the capacity to deliver 1.1 mg, 21.8 mg, and 4 mg to the mouth, stomach, and duodenum during 18 h, respectively. This is a pioneering study since the carriers were intelligently developed to improve CBD release.

show abstract

Predicting Dissolution of Entecavir Using the Noyes Whitney Equation

Cited by 2 publications

References 17 publications

Nanoliposomes for Controlled Release of Cannabinodiol at Relevant Gastrointestinal Conditions

Nanoliposomes for Controlled Release of Cannabinodiol at Relevant Gastrointestinal Conditions

Bioactive Properties and In Vitro Digestive Release of Cannabidiol (CBD) from Tailored Composites Based on Carbon Materials

Contact Info

Product

Resources

About