Untitled

Rinaki, Eleni; Dokoumetzidis, Aristides; Macheras, Panos

doi:10.1023/a:1022652004114

Cited by 67 publications

(9 citation statements)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…MDT reflects the time for the drug to dissolve and is the first statistical moment for the cumulative dissolution process and provides an accurate drug‐release rate. A higher MDT value indicates a greater drug‐release‐retarding ability 39. MDT 50% was calculated according to eq.…”

Section: Resultsmentioning

confidence: 99%

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al³⁺–alginate hydrogel network: In vitro and in vivo performance

Dey

Maiti²,

2012

J of Applied Polymer Sci

View full text Add to dashboard Cite

Sodium alginate and carboxymethyl locust bean gum (CMLBG) were reticulated in an aqueous solution of AlCl 3 , and this novel interpenetrating network (IPN) hydrogel encapsulated about 93-98% glipizide. The degree of reticulation in the spherical IPN beads was confirmed by Fourier transform infrared spectroscopy, elemental analysis, neutralization equivalent determination, tensile strength testing, and differential scanning calorimetry analysis. An increase in the CMLBG weight ratio and the degree of crosslinking in the IPN was found to increase mean dissolution time of the encapsulated drug. The dissolution efficiency was found to be much higher in the medium at pH 7.4 than at pH 1.2. The swelling of IPN depended on the pH of the medium, and accordingly, monitored the drug release for a period of 8 h. The anomalous drug transport mechanism was presumed to be operative. High performance liquid chromatography (HPLC) analysis showed the drug's stability in the IPN during encapsulation. The IPN showed significant hypoglycemic activity on male Wistar rats for up to 10 h. This could be beneficial for diabetic patients for achieving control over blood glucose levels.

show abstract

Section: Resultsmentioning

confidence: 99%

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al³⁺–alginate hydrogel network: In vitro and in vivo performance

Dey

Maiti²,

2012

J of Applied Polymer Sci

View full text Add to dashboard Cite

show abstract

“…While MDT is kinetic parameter used to characterize drug release rate and indicate drug release retarding efficiency of polymers used. It depends on dose/solubility ratio [75].…”

Section: Discussionmentioning

confidence: 99%

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

et al. 2020

View full text Add to dashboard Cite

Targeted drug delivery offers great opportunities for treating cancer. Here, we developed a novel anticancer targeted delivery system for piperine (Pip), an alkaloid prodrug derived from black pepper that exhibits anticancer effects. The tailored delivery system comprises aggregated hydroxyapatite nanoparticles (HAPs) functionalized with phosphonate groups (HAP-Ps). Pip was loaded into HAPs and HAP-Ps at pH 7.2 and 9.3 to obtain nanoformulations. The nanoformulations were characterized using several techniques and the release kinetics and anticancer effects investigated in vitro. The Pip loading capacity was >20%. Prolonged release was observed with kinetics dependent on pH, surface modification, and coating. The nanoformulations fully inhibited monolayer HCT116 colon cancer cells compared to Caco2 colon cancer and MCF7 breast cancer cells after 72 h, whereas free Pip had a weaker effect. The nanoformulations inhibited ~60% in HCT116 spheroids compared to free Pip. The Pip-loaded nanoparticles were also coated with gum Arabic and functionalized with folic acid as a targeting ligand. These functionalized nanoformulations had the lowest cytotoxicity towards normal WI-38 fibroblast cells. These preliminary findings suggest that the targeted delivery system comprising HAP aggregates loaded with Pip, coated with gum Arabic, and functionalized with folic acid are a potentially efficient agent against colon cancer.

show abstract

Section: The Evolution Of Gi Drug Absorption Analysismentioning

confidence: 99%

“…It should be noted that dissolution specifications of the FDA guidance are not correlated with the drug’s solubility/dose ratio, which has been shown to control the rate of drug dissolution 39. It was Lansky and Weis40 who raised a question on this issue for the first time in 1999, and soon after dose was incorporated explicitly into the fundamental relationships used routinely in dissolution 39. 41 The Noyes–Whitney equation (Equation 1) was modified taking into account the dose and the volume of the dissolution medium;39, 41 thus Equation 1 was expressed in terms of the fraction of dose dissolved, Φ : …”

Section: The Evolution Of Gi Drug Absorption Analysismentioning

confidence: 99%

“…where k is the dissolution rate constant and q is the dimensionless dose/aqueous solubility ( C s ) ratio since the volume of the dissolution medium, V has been taken into account ( q =dose /C s ⋅ V ) 39. Equation 2 reveals that 1/ q is the primary parameter for the rate of drug dissolution in terms of Φ ; this was one of the reasons justifying the recent use of 1/ q in the quantitative‐BCS 42.…”

Section: The Evolution Of Gi Drug Absorption Analysismentioning

confidence: 99%

See 1 more Smart Citation

Computational‐Regulatory Developments in the Prediction of Oral Drug Absorption

Valsami

Macheras

2011

Molecular Informatics

View full text Add to dashboard Cite

Early prediction of human intestinal absorption is important in selection of potential orally administered drugs. Various computational models for prediction of the fraction of dose absorbed, Fa, have been developed. In 1989, a sigmoidal relationship between Fa and drug absorption potential was shown. Since then various physicochemical descriptors of molecules (lipophilicity, polar surface area, hydrogen bond descriptors) have been found to correlate with human intestinal absorption and various attempts in estimating Fa have been reported. Most studies rely on the presupposition that Fa is mainly dependent on drug's solubility, which drives the dissolution rate in the gastrointestinal (GI) fluids, and the rate of passive drug transport across the intestinal membrane. In the same vein, the biopharmaceutics classification system (BCS) and the relevant FDA guideline classify drugs in four categories according to their aqueous solubility and permeability. However, the biopharmaceutics drug disposition classification system (BDDCS) revealed the poor predictability of permeability estimates for Fa and the major role of transporters for GI uptake of drugs. The role of solubility in the reaction limited model of dissolution and the ubiquitous presence of supersaturated solubility-dissolution phenomena in the GI lumen, call for a more physiologically relevant consideration of GI absorption.

show abstract

Untitled

Abstract: The mean dissolution time of a drug depends on dose/ solubility ratio, even when the model considered is the simplest possible. This fact plays an important role in drug absorption when absorption is dissolution limited.

Cited by 67 publications

References 10 publications

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al³⁺–alginate hydrogel network: In vitro and in vivo performance

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al³⁺–alginate hydrogel network: In vitro and in vivo performance

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

Computational‐Regulatory Developments in the Prediction of Oral Drug Absorption

Contact Info

Product

Resources

About

Untitled

Abstract: The mean dissolution time of a drug depends on dose/ solubility ratio, even when the model considered is the simplest possible. This fact plays an important role in drug absorption when absorption is dissolution limited.

Cited by 67 publications

References 10 publications

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al3+–alginate hydrogel network: In vitro and in vivo performance

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al3+–alginate hydrogel network: In vitro and in vivo performance

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

Computational‐Regulatory Developments in the Prediction of Oral Drug Absorption

Contact Info

Product

Resources

About

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al³⁺–alginate hydrogel network: In vitro and in vivo performance

Gastrointestinal delivery of glipizide from carboxymethyl locust bean gum–Al³⁺–alginate hydrogel network: In vitro and in vivo performance