scholarly journals A Review of Pharmaceutical Nano-Cocrystals: A Novel Strategy to Improve the Chemical and Physical Properties for Poorly Soluble Drugs

Crystals ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 463
Author(s):  
Jianbing Tan ◽  
Jianhao Liu ◽  
Liling Ran

Nowadays, many commercial drugs have poor solubility and bioavailability. Cocrystals are formulated to modulate active pharmaceutical ingredients’ properties with improved solubility, dissolution, and bioavailability compared to their pristine individual components in the pharmaceutical industry. Nano-cocrystals, crystals in the nano range, can further enhance these properties because of not only the cocrystal structure, but also the large surface to volume ratio of nanocrystals. Even though there are many studies on cocrystals, the research of pharmaceutical nano-cocrystals is still in the initial stage. Thus, it is necessary to conduct a systematic study on pharmaceutical nano-cocrystals. In this review, the possible preparation approaches of nano-cocrystals have been reported. To have a comprehensive understanding of nano-cocrystals, some analytical techniques and characterizations will be discussed in detail. In addition, the feasible therapeutic application of nano-cocrystals will be presented. This work is expected to provide guidance to develop new nano-cocrystals with commercial value in the pharmaceutical industry.

Polymers ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 929 ◽  
Author(s):  
Miguel Gómez-Ballesteros ◽  
José Javier López-Cano ◽  
Irene Bravo-Osuna ◽  
Rocío Herrero-Vanrell ◽  
Irene Teresa Molina-Martínez

The combination of acetazolamide-loaded nano-liposomes and Hydroxypropyl methylcellulose (HPMC) with similar components to the preocular tear film in an osmoprotectant media (trehalose and erythritol) is proposed as a novel strategy to increase the ocular bioavailability of poorly soluble drugs. Ophthalmic formulations based on acetazolamide-loaded liposomes, dispersed in the osmoprotectant solution (ACZ-LP) or in combination with HPMC (ACZ-LP-P) were characterized and in vivo evaluated. The pH and tonicity of both formulations resulted in physiological ranges. The inclusion of HPMC produced an increment in viscosity (from 0.9 to 4.7 mPa·s. 64.9 ± 2.6% of acetazolamide initially included in the formulation was retained in vesicles. In both formulations, a similar onset time (1 h) and effective time periods were observed (7 h) after a single instillation (25 μL) in normotensive rabbits’ eyes. The AUC0–8h of the ACZ-LP-P was 1.5-fold higher than of ACZ-LP (p < 0.001) and the maximum hypotensive effect resulted in 1.4-fold higher (p < 0.001). In addition, the formulation of ACZ in the hybrid liposome/HPMC system produced a 30.25-folds total increment in ocular bioavailability, compared with the drug solution. Excellent tolerance in rabbits’ eyes was confirmed during the study.


2019 ◽  
Vol 9 (01) ◽  
pp. 15-20
Author(s):  
B Pandey ◽  
A B Khan

The aim of the review was to explore the necessity, advantages and different techniques of oral films for enhancing solubility of poorly soluble drugs with an emphasis on the newer, state-of the art technologies, such as 3D printing and hot-melt extrusion (HME). The historical background of oral films is presented along with the regularly used techniques. The modern approach of quality-by-design (QbD) is unravelled, identifying appropriate critical process parameters (CPP) and applied to oral films. A section is devoted modern technologies such as 3D printing and HME of oral films. Oral films are innovative formulations by which poorly soluble drugs have been founds to give positive results in enhancing their solubility and dissolution characteristics. With modern sophisticated techniques, precise mass production of oral films has been given a thrust. Oral films have better patient compliance, improved biopharmaceutical properties, improved efficacy, and better safety. By applying QbD and implementation of modern technologies the newer generation of oral films are yielding promising results


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.


Lab on a Chip ◽  
2021 ◽  
Author(s):  
Peer Erfle ◽  
Juliane Riewe ◽  
Heike Bunjes ◽  
Andreas Dietzel

Poorly soluble drugs can be incorporated in lipid carrier nanoparticles to achieve sufficient bioavailability and open up diverse routes of administration. Preparation by antisolvent precipitation in microfluidic systems enables excellent...


Author(s):  
Adryana Rocha Clementino ◽  
Giulia Pellegrini ◽  
Sabrina Banella ◽  
Gaia Colombo ◽  
Laura Cantù ◽  
...  

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