Nanonization techniques to overcome poor water-solubility with drugs

2020 ◽  
Vol 15 (7) ◽  
pp. 853-864
Author(s):  
Flávia Lidiane Oliveira Da Silva ◽  
Maria Betânia De Freitas Marques ◽  
Kelly Cristina Kato ◽  
Guilherme Carneiro
2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan

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.


RSC Advances ◽  
2015 ◽  
Vol 5 (84) ◽  
pp. 68743-68750 ◽  
Author(s):  
Sacheen Kumar ◽  
Jaspreet Kaur Randhawa

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.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1372
Author(s):  
Chun-Yin Yang ◽  
Pao-Hsien Huang ◽  
Chih-Hua Tseng ◽  
Feng-Lin Yen

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.


Author(s):  
Jiahao Huang ◽  
◽  
Shawn Wettig

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.


2007 ◽  
Vol 59 (7) ◽  
pp. 677-694 ◽  
Author(s):  
Valentino J. Stella ◽  
Kwame W. Nti-Addae

2015 ◽  
Vol 78 (1) ◽  
pp. 22-30 ◽  
Author(s):  
SHENGFENG PENG ◽  
LIQIANG ZOU ◽  
WEI LIU ◽  
LU GAN ◽  
WEILIN LIU ◽  
...  

Eugenol is a major phenolic component with diverse biological activities. However, it is difficult to formulate into an aqueous solution due to poor water solubility, and this limits its application. In the present study, eugenol nanoliposomes (EN) were prepared by combining the ethanol injection method with the dynamic high-pressure microfluidization method. Good physicochemical characterizations of EN were obtained. The successful encapsulation of eugenol in nanoliposomes was confirmed by Fourier transform infrared spectroscopy. A good storage stability of EN was confirmed by its low variation of average particle diameter and encapsulation efficiency after 8 weeks of storage. No oil drops were found in EN after 8 weeks of storage at 4°C and at room temperature, which suggested that the poor water solubility of eugenol was overcome by nanoliposome encapsulation. Compared with that of eugenol solution, a relatively good sustained release property was observed in EN. The antibacterial activity of EN against four common foodborne pathogenic bacteria (Staphylococcus aureus, Escherichia coli, Salmonella enterica serovar Typhimurium, and Listeria monocytogenes) was evaluated in both Luria broth and milk medium.


2019 ◽  
Vol 9 (6) ◽  
pp. 17-22
Author(s):  
Moumita Paul ◽  
Pintu Sarkar ◽  
Riyanka Sengupta ◽  
Saikat Bhunia ◽  
Payal Jana ◽  
...  

Modern drug discovery has led to the development of drug molecules that exhibit high lipophilicity and poor water solubility, which leads to problematic bioavailability. Approaches have thus been made to enhance dissolution of poorly water soluble drugs through modifications and creation of specific formulations. Metaclopramide is an antiemetic and gastroprokinetic agent, commonly used to treat nausea and vomiting. It is absorbed well after oral administration but a significant first pass effect in some human patients may reduce systemic bioavailability to 30%.The Metaclopramide base is thus modified from Metaclopramide hydrochloride to enhance solubility .This has been achieved by the formulating in solid dispersion since Metaclopramide is poorly water soluble. Though it is absorbed well after oral administration, a significant first pass effect in some patients reduces systemic bioavailability, which can cause adverse side effects. This solid dispersion has then been used through transdermal drug delivery. Enhancement of solubility of poorly water soluble drug by solid dispersion may be attributed to particles modified characters such as particle size reduction, improved wettability, higher porosity, decreased lattice energy, amorphous state. The main objective thus includes modification of drug Metaclopramide  hydrochloride to Metaclopramide base, preparation of solid dispersion of modified Metaclopramide  base drug which has poor water solubility, experimental analysis of Metaclopramide base drug and solid dispersion products with carriers. Keywords: solubility, Metaclopramide, solid dispersion, carriers, HPβCD, PVP K-30


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