scholarly journals A New Strategy for Enhancing the Oral Bioavailability of Drugs with Poor Water-Solubility and Low Liposolubility Based on Phospholipid Complex and Supersaturated SEDDS

PLoS ONE ◽  
2013 ◽  
Vol 8 (12) ◽  
pp. e84530 ◽  
Author(s):  
Hui Zhou ◽  
Jiangling Wan ◽  
Lei Wu ◽  
Tao Yi ◽  
Wei Liu ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Water Solubility ◽  
Phospholipid Complex ◽  
New Strategy ◽  
Poor Water Solubility

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

scholarly journals Enhanced Water Solubility and Oral Bioavailability of Paclitaxel Crystal Powders through an Innovative Antisolvent Precipitation Process: Antisolvent Crystallization Using Ionic Liquids as Solvent

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1008 ◽  
Author(s):  
Qilei Yang ◽  
Chang Zu ◽  
Wengang Li ◽  
Weiwei Wu ◽  
Yunlong Ge ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
High Performance ◽  
Water Solubility ◽  
Water Soluble ◽  
Precipitation Process ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Antisolvent Precipitation ◽  
Antisolvent Crystallization ◽  
Artificial Gastric Juice

Paclitaxel (PTX) is a poor water-soluble antineoplastic drug with significant antitumor activity. However, its low bioavailability is a major obstacle for its biomedical applications. Thus, this experiment is designed to prepare PTX crystal powders through an antisolvent precipitation process using 1-hexyl-3-methylimidazolium bromide (HMImBr) as solvent and water as an antisolvent. The factors influencing saturation solubility of PTX crystal powders in water in water were optimized using a single-factor design. The optimum conditions for the antisolvent precipitation process were as follows: 50 mg/mL concentration of the PTX solution, 25 °C temperature, and 1:7 solvent-to-antisolvent ratio. The PTX crystal powders were characterized via scanning electron microscopy, Fourier transform infrared spectroscopy, high-performance liquid chromatography–mass spectrometry, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Raman spectroscopy, solid-state nuclear magnetic resonance, and dissolution and oral bioavailability studies. Results showed that the chemical structure of PTX crystal powders were unchanged; however, precipitation of the crystalline structure changed. The dissolution test showed that the dissolution rate and solubility of PTX crystal powders were nearly 3.21-folds higher compared to raw PTX in water, and 1.27 times higher in artificial gastric juice. Meanwhile, the bioavailability of PTX crystal increased 10.88 times than raw PTX. These results suggested that PTX crystal powders might have potential value to become a new oral PTX formulation with high bioavailability.

Solid lipid nanoparticles of stearic acid for the drug delivery of paliperidone

RSC Advances ◽  
2015 ◽  
Vol 5 (84) ◽  
pp. 68743-68750 ◽  
Author(s):  
Sacheen Kumar ◽  
Jaspreet Kaur Randhawa
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Antipsychotic Drug ◽  
Solid Lipid Nanoparticles ◽  
Water Solubility ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Poor Water Solubility

Paliperidone is an antipsychotic drug having poor water solubility and bioavailability. Solid lipid nanoparticles of stearic acid loaded with paliperidone were prepared to enhance the bioavailability.

scholarly journals Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1372
Author(s):  
Chun-Yin Yang ◽  
Pao-Hsien Huang ◽  
Chih-Hua Tseng ◽  
Feng-Lin Yen
Keyword(s):  
Water Solubility ◽  
Methanol Extract ◽  
Biological Effects ◽  
Skin Permeation ◽  
Environmental Pollutants ◽  
Skin Penetration ◽  
Physicochemical Characteristics ◽  
The Poor ◽  
Deep Layers ◽  
Poor Water Solubility

Antioxidants from plant extracts are often used as additives in skincare products to prevent skin problems induced by environmental pollutants. Artocarpus communis methanol extract (ACM) has many biological effects, such as antioxidant, anti-inflammatory, wound healing, and photoprotective effects; however, the poor water solubility of raw ACM has limited its applications in medicine and cosmetics. Topical antioxidant nanoparticles are one of the drug-delivery systems for overcoming the poor water solubility of antioxidants for increasing their skin penetration. The present study demonstrated that ACM-loaded hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone K30 nanoparticles (AHP) were successfully prepared and could effectively increase the skin penetration of ACM through changing the physicochemical characteristics of raw ACM, including reducing the particle size, increasing the surface area, and inducing amorphous transformation. Our results also revealed that AHP had significantly better antioxidant activity than raw ACM for preventing photocytotoxicity because the AHP formulation increased the cellular uptake of the ACM in UVB-irradiated HaCaT keratinocytes. In conclusion, our results suggest that AHP may be used as a good topical antioxidant nanoparticle for delivering ACM into deep layers of the skin for preventing UVB-induced skin problems.

Phospholipid-containing films for improved drug release

2021 ◽  
pp. 30-33
Author(s):  
Jiahao Huang ◽  
◽  
Shawn Wettig
Keyword(s):  
Water Solubility ◽  
Aqueous Media ◽  
Active Pharmaceutical Ingredients ◽  
Natural Sources ◽  
Pharmaceutical Ingredients ◽  
Alternative Approach ◽  
Poor Water Solubility ◽  
Dissolution Efficiency ◽  
Oral Films ◽  
Liquid Liquid Phase Separation

Phospholipids from natural sources can delay liquid-liquid phase separation and improve supersaturation for active pharmaceutical ingredients with poor water-solubility in aqueous media. Researchers have developed oral films containing phospholipids to enhance the dissolution efficiency of hydrophobic pharmaceutical ingredients. Phospholipid-based oral films provide an alternative approach for compounding pharmacies to formulate drugs with poor water solubility.

scholarly journals Enhanced Oral Bioavailability, Anti-Tumor Activity and Hepatoprotective Effect of 6-Shogaol Loaded in a Type of Novel Micelles of Polyethylene Glycol and Linoleic Acid Conjugate

Pharmaceutics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 107 ◽  
Author(s):  
Huiyun Zhang ◽  
Qilong Wang ◽  
Congyong Sun ◽  
Yuan Zhu ◽  
Qiuxuan Yang ◽  
...  
Keyword(s):  
Linoleic Acid ◽  
Oral Bioavailability ◽  
Water Solubility ◽  
Oral Absorption ◽  
Treatment Effectiveness ◽  
Hepatoprotective Effect ◽  
Nanoprecipitation Method ◽  
Acid Conjugate

：6-shogaol is a promising anti-cancer and anti-inflammatory agent. However, the treatment effectiveness of 6-shogaol is limited by poor water solubility, poor oral absorption and rapid metabolism. Herein, 6-shogaol loaded in micelles (SMs) were designed to improve 6-shogaol’s solubility and bioavailability. The micelles of a PEG derivative of linoleic acid (mPEG2k-LA) were prepared by the nanoprecipitation method with a particle size of 76.8 nm, and entrapment of 81.6 %. Intriguingly, SMs showed a slower release in phosphate buffer saline (PBS) (pH = 7.4) compared to free 6-shogaol while its oral bioavailability increased by 3.2–fold in vivo. More importantly, the in vitro cytotoxic effect in HepG2 cells of SMs was significantly higher than free 6-shogaol. Furthermore, SMs could significantly improve the tissue distribution of 6-shogaol, especially liver and brain. Finally, SMs showed a better hepatoprotective effect against carbon tetrachloride (CCl4)-induced hepatic injury in vivo than free 6-shogaol. These results suggest that the novel micelles could potentiate the activities of 6-shogaol in cancer treatment and hepatoprotection.

A novel nanosized phospholipid complex of Biochanin A for improving oral bioavailability: Preparation and in-vitro/in-vivo characterizations

2021 ◽  
Vol 61 ◽  
pp. 102254
Author(s):  
Sandeep Kumar Singh ◽  
Mamunur Rashid ◽  
Kripal Bhalala ◽  
Yaseen Malik ◽  
Swati Chaturvedi ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Biochanin A ◽  
Phospholipid Complex
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