scholarly journals Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment

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
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Tear Film ◽  
Onset Time ◽  
Hypotensive Effect ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble ◽  
Ocular Bioavailability ◽  
Novel Strategy ◽  
Drug Solution

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.

In vitro -in vivo correlation in the effect of cyclodextrin on oral absorption of poorly soluble drugs

2021 ◽  
pp. 120494
Author(s):  
Risa Aihara ◽  
Roman Messerschmid ◽  
Masashi Mizoguchi ◽  
Koichi Wada ◽  
Keiko Minami ◽  
...  
Keyword(s):  
Oral Absorption ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

scholarly journals Modern Evaluation of Liquisolid Systems with Varying Amounts of Liquid Phase Prepared Using Two Different Methods

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Barbora Vraníková ◽  
Jan Gajdziok ◽  
David Vetchý
Keyword(s):  
Liquid Phase ◽  
Dosage Form ◽  
Polyethylene Glycol 400 ◽  
Fluid Bed ◽  
Poorly Soluble ◽  
Hardness Values ◽  
Specific Evaluation ◽  
Drug Solution

Liquisolid systems are an innovative dosage form used for enhancing dissolution rate and improvingin vivobioavailability of poorly soluble drugs. These formulations require specific evaluation methods for their quality assurance (e.g., evaluation of angle of slide, contact angle, or water absorption ratio). The presented study is focused on the preparation, modernin vitrotesting, and evaluation of differences of liquisolid systems containing varying amounts of a drug in liquid state (polyethylene glycol 400 solution of rosuvastatin) in relation to an aluminometasilicate carrier (Neusilin US2). Liquisolid powders used for the formulation of final tablets were prepared using two different methods: simple blending and spraying of drug solution onto a carrier in fluid bed equipment. The obtained results imply that the amount of liquid phase in relation to carrier material had an effect on the hardness, friability, and disintegration of tablets, as well as their height. The use of spraying technique enhanced flow properties of the prepared mixtures, increased hardness values, decreased friability, and improved homogeneity of the final dosage form.

Ocular delivery systems for poorly soluble drugs: An in-vivo evaluation

2013 ◽  
Vol 455 (1-2) ◽  
pp. 331-337 ◽  
Author(s):  
C. Luschmann ◽  
W. Herrmann ◽  
O. Strauß ◽  
K. Luschmann ◽  
A. Goepferich
Keyword(s):  
Delivery Systems ◽  
Poorly Soluble Drugs ◽  
Ocular Delivery ◽  
In Vivo Evaluation ◽  
Poorly Soluble

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
Keyword(s):  
Pharmaceutical Industry ◽  
Volume Ratio ◽  
Analytical Techniques ◽  
Poorly Soluble Drugs ◽  
Therapeutic Application ◽  
Pharmaceutical Ingredients ◽  
Initial Stage ◽  
Poorly Soluble ◽  
Novel Strategy ◽  
Cocrystal Structure

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.

Soluplus® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo

2012 ◽  
Vol 45 (3) ◽  
pp. 336-343 ◽  
Author(s):  
Michael Linn ◽  
Eva-Maria Collnot ◽  
Dejan Djuric ◽  
Katja Hempel ◽  
Eric Fabian ◽  
...  
Keyword(s):  
Absorption Enhancer ◽  
Poorly Soluble Drugs ◽  
Effective Absorption ◽  
Poorly Soluble

Technological Advancements in Oral Films

2019 ◽  
Vol 9 (01) ◽  
pp. 15-20
Author(s):  
B Pandey ◽  
A B Khan
Keyword(s):  
3D Printing ◽  
Historical Background ◽  
Poorly Soluble Drugs ◽  
Modern Approach ◽  
Poorly Soluble ◽  
Critical Process Parameters ◽  
Biopharmaceutical Properties ◽  
Oral Films ◽  
Hot Melt ◽  
Modern Technologies

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

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