Property prediction and pharmacokinetic evaluation of mixed stoichiometry cocrystals of zafirlukast, a drug delivery case study

CrystEngComm ◽  
2018 ◽  
Vol 20 (10) ◽  
pp. 1346-1351 ◽  
Author(s):  
Philip A. Corner ◽  
David J. Berry ◽  
James F. McCabe ◽  
Rafael Barbas ◽  
Rafel Prohens ◽  
...  

Cocrystals have been identified as a method for ensuring the delivery of poorly soluble drugs.

2019 ◽  
Vol 15 (6) ◽  
pp. 576-588 ◽  
Author(s):  
Beibei Yan ◽  
Yu Gu ◽  
Juan Zhao ◽  
Yangyang Liu ◽  
Lulu Wang ◽  
...  

: According to the drug discovery, approximately 40% of the new chemical entities show poor bioavailability due to their low aqueous solubility. In order to increase the solubility of the drugs, self-micro emulsifying drug delivery systems (SMEDDS) are considered as an ideal technology for enhancing the permeability of poorly soluble drugs in GI membranes. The SMEDDS are also generally used to enhance the oral bioavailability of the hydrophobic drugs. At present, most of the self-microemulsion drugs are liquid dosage forms, which could cause some disadvantages, such as the low bioavailability of the traditional liquid SMEDDS. Therefore, solid self-micro emulsifying drug delivery systems (S-SMEDDS) have emerged widely in recent years, which were prepared by solidifying a semi-solid or liquid self-emulsifying (SE) ingredient into a powder in order to improve stability, treatment and patient compliance. The article gives a comprehensive introduction of the study of SMEDDS which could effectively tackle the problem of the water-insoluble drug, especially the development of solidification technology of SMEDDS. Finally, the present challenges and the prospects in this field were also discussed.


2017 ◽  
Vol 1479 ◽  
pp. 161-168 ◽  
Author(s):  
Justine Thiry ◽  
Brigitte Evrard ◽  
Gwenaël Nys ◽  
Marianne Fillet ◽  
Miranda G.M. Kok

2019 ◽  
Vol 13 (2) ◽  
pp. 91-104 ◽  
Author(s):  
Surya Goel ◽  
Monika Sachdeva ◽  
Vijay Agarwal

Background: Nanosuspension has arisen as a remunerative, lucrative as well as a potent approach to improve the solubility and bioavailability of poorly aqueous soluble drug entities. Several challenges are still present in this approach which need more research. The prime aim of this review is to identify such challenges that can be rectified in the future. Methods: Through this review, we enlighten the recent patents and advancement in nanosuspension technology that utilize the different drug moieties, instruments and characterization parameters. Results: Nanosuspension has been found to possess great potential to rectify the several issues related to poor bioavailability, site-specific drug delivery, dosing frequency, etc. In the past decade, nanosuspension approach has been complementarily utilized to solve the developed grievances, arisen from poorly soluble drugs. But this field still needs more attention to new discoveries. Conclusion: Nanosuspension contributes a crucial role in administering the different drug entities through a variety of routes involving oral, transdermal, ocular, parenteral, pulmonary, etc. with solving the different issues. This review also confirms the significance of nanosuspension in safety, efficacy, and communal as well as the economic expense associated with healthcare.


2016 ◽  
Vol 13 (10) ◽  
pp. 3417-3426 ◽  
Author(s):  
P. J. Sassene ◽  
M. H. Michaelsen ◽  
M. D. Mosgaard ◽  
M. K. Jensen ◽  
E. Van Den Broek ◽  
...  

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 134 ◽  
Author(s):  
Maria Gigliobianco ◽  
Cristina Casadidio ◽  
Roberta Censi ◽  
Piera Di Martino

Many approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of “pure drugs and a minimum of surface active agents required for stabilization”. They are defined as “carrier-free submicron colloidal drug delivery systems with a mean particle size in the nanometer range, typically between 10–800 nm”. The primary importance of these nanoparticles was the reduction of particle size to nanoscale dimensions, with an increase in the particle surface area in contact with the dissolution medium, and thus in bioavailability. This approach has been proven successful, as demonstrated by the number of such drug products on the market. Nonetheless, despite the definition that indicates nanocrystals as a “carrier-free” system, surface active agents are necessary to prevent colloidal particles aggregation and thus improve stability. In addition, in more recent years, nanocrystal properties and technologies have attracted the interest of researchers as a means to obtain colloidal particles with modified biological properties, and thus their interest is now also addressed to modify the drug delivery and targeting. The present work provides an overview of the achievements in improving the bioavailability of poorly soluble drugs according to their administration route, describes the methods developed to overcome physicochemical and stability-related problems, and in particular reviews different stabilizers and surface agents that are able to modify the drug delivery and targeting.


2019 ◽  
Vol 20 (2) ◽  
Author(s):  
Georgios K. Eleftheriadis ◽  
Panagiota Mantelou ◽  
Christina Karavasili ◽  
Paschalina Chatzopoulou ◽  
Dimitrios Katsantonis ◽  
...  

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