Untitled

doi:10.13040/ijpsr.0975-8232.2(10).2501-13

Cited by 4 publications

(3 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Solid dispersion (SD) is another popular solubilizing technology for oral products. , A mixture of drugs and hydrophilic polymers is treated with solvent evaporation such as spray drying or melting–extrusion, and drug molecules are rapidly solidified in the polymer matrix to generate an amorphous state rather than a crystalline form. Amorphous drugs have higher free energy and higher solubility than their crystalline form and dissolve more rapidly, while polymers prevent nucleation of the drug crystals in the gastrointestinal fluid, known as supersaturation.…”

Section: Amount-controlled Ddsmentioning

confidence: 99%

Oral Drug Delivery Systems Applied to Launched Products: Value for the Patients and Industrial Considerations

Yoshida,

Kojima

2023

Mol. Pharmaceutics

View full text Add to dashboard Cite

Drug delivery systems (DDS) control the amount, rate, and site of administration of drug substances in the body as well as their release and ADME (absorption, distribution, metabolism, excretion). Among the various types of DDS, amount-controlled DDS for solubilization and absorption increase the bioavailability. Time-and amount-controlled DDS are controlled release formulations classified as (1) membrane-type, (2) matrix-type, (3) osmotic-type, and (4) ion-exchange type. Timed-release formulations also control the time and amount of release and the absorption of drugs. Site-and amount-controlled DDS are characterized by colonic delivery and intestinal lymphtargeting to improve release and ADME of drug substances. Finally, site-, time-, and amount-controlled DDS are gastroretentive formulations and local delivery in the oral cavity to improve site retention, release, and ADME of drugs. DDS can enhance efficacy, reduce adverse effects, and optimize the dosing frequency of various drug products to increase patient value. This review focuses on patient value and industrial considerations of launched oral DDS. We provide a technological overview of candidate and marketed DDS, as well as the pros/cons of the technologies for industrialization with consideration to excipients, manufacturing, and storage stability. Moreover, to demonstrate the usefulness of the technology and support the selection and development of the best technologies for patients, we also describe patient value from clinical studies and analyses, particularly with regard to increased new medical options, higher efficacy, reduced adverse effects, reduced number of doses and clinic visits, easier administration, higher quality of life, greater adherence, and satisfaction.

show abstract

Section: Amount-controlled Ddsmentioning

confidence: 99%

Oral Drug Delivery Systems Applied to Launched Products: Value for the Patients and Industrial Considerations

Yoshida,

Kojima

2023

Mol. Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…Thus, the solubility enhancement of API in water has become a pivotal focus within pharmaceutical research and development . Several techniques can be utilized to improve the solubility of APIs with low solubility in water, − such as chemically modifying the API’s structure, using hydrotropes, , cosolvents and surfactants, polymeric micelles, encapsulation, inclusion complexes, solid dispersion to maintain the API in an amorphous state, polymorphism, micronization or nanonization, , cocrystallization, and eutectic mixtures formation . Enhancing the API solubility via the formation of eutectic mixtures is a straightforward method realized by mixing the API with an excipient.…”

Section: Introductionmentioning

confidence: 99%

Revealing the Solubility Enhancement of Active Pharmaceutical Ingredients through Eutectic Mixtures Formation: A Parameter Study

Nasrallah,

Alhadid,

Minceva

2024

Crystal Growth & Design

View full text Add to dashboard Cite

The active pharmaceutical ingredient (API) solubility is critical for their bioavailability, dosing precision, stability, and overall efficacy. Forming eutectic mixtures between an API and an excipient has been widely used to improve API solubility. However, from a thermodynamic perspective, this approach is still relatively underexplored. This study explores the parameters influencing the solubility enhancement of an API with poor solubility in water by eutectic mixture formation. A hypothetical ternary system consisting of an API, excipient, and water was considered. The study investigated the impact of excipient melting properties and molecular interactions among the API, excipient, and water on API solubility in water. The two-suffix Margules equation was used to model the liquid phase nonideality. The study revealed that strong API−excipient and excipient−water interactions notably enhanced API solubility in water. However, this effect was counteracted when excipient−water interactions surpassed API−excipient interactions in strength. Additionally, the melting properties of the excipient had a significant influence on the composition of the mixture at the eutectic point and API solubility enhancement factor. This research underscores the essential characteristics a potential excipient should possess to maximize API solubility in water and other solvents. The results emphasize the importance of eutectic mixture formation in addressing the challenges associated with water-insoluble APIs.

show abstract

“…Nanoencapsulation involves the formation of particles with diameters between 1 and 1 000 nm that are loaded with active ingredients . Compared to microsized particles, nanoparticles (NPs) can provide more surface area and enhance solubility and bioavailability . In addition, the high ratio of surface area to volume of nanoencapsulation systems can be used to establish an adhesive interaction between NPs and mucus or mucin. , …”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Mucoadhesive Nanoparticles for Enhancing Cellular Uptake of Coenzyme Q10

Lee

Suh

Kim

et al. 2017

J. Agric. Food Chem.

View full text Add to dashboard Cite

The mucoadhesive nanoparticles (NPs) for oral delivery of coenzyme Q10 (CoQ10) were prepared using natural mucoadhesive polysaccharides, chitosan (CS), and dextran sulfate sodium salt (DS) in order to improve the solubility, cellular uptake, and thermo- and photostability of CoQ10. CoQ10-loaded NPs were prepared in the range of 340-450 nm with an entrapment efficiency of 60-98%. The mucoadhesiveness and cellular uptake of NPs were evaluated by measuring the amount of mucin adsorbed on NPs and CoQ10 absorbed in Caco-2 cells, respectively. CS/DS NPs had higher mucoadhesive strength than CS/sodium triphosphate pentabasic NPs (control group). Moreover, the solubility, cellular uptake, thermo- and photostability of CS/DS NPs were significantly improved compared with non-nanoencapsulated free CoQ10. Particularly, CS/DS NPs prepared with 0.5 mg/mL of CS and DS produced the highest mucoadhesiveness, solubility, cellular uptake, and cellular antioxidant activity. Thus, mucoadhesive CS/DS NPs may be an effective oral delivery platform for improving bioavailability of CoQ10.

show abstract

Untitled

Cited by 4 publications

References 37 publications

Oral Drug Delivery Systems Applied to Launched Products: Value for the Patients and Industrial Considerations

Oral Drug Delivery Systems Applied to Launched Products: Value for the Patients and Industrial Considerations

Revealing the Solubility Enhancement of Active Pharmaceutical Ingredients through Eutectic Mixtures Formation: A Parameter Study

Preparation and Characterization of Mucoadhesive Nanoparticles for Enhancing Cellular Uptake of Coenzyme Q10

Contact Info

Product

Resources

About