Transdermal delivery of rapamycin with poor water-solubility by dissolving polymeric microneedles for anti-angiogenesis

2020 ◽  
Vol 8 (5) ◽  
pp. 928-934 ◽  
Author(s):  
Jinzhu Mao ◽  
Hua Wang ◽  
Ying Xie ◽  
Yangxue Fu ◽  
Yuce Li ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Water Solubility ◽  
Dissolving Microneedles ◽  
The Matrix ◽  
Angiogenic Effect ◽  
Poor Water Solubility

Rapamycin-loaded dissolving microneedles (RAPA DMNs) are fabricated by using polyvinylpyrrolidone (PVP) as the matrix and exhibit the good anti-angiogenic effect.

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.

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 Extracted Compounds from Neem Leaves as Antimicrobial Agent on the Physico-Chemical Properties of Seaweed-Based Biopolymer Films

Polymers ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 1119 ◽  
Author(s):  
U. Seeta Uthaya Kumar ◽  
S. N. Abdulmadjid ◽  
N. G. Olaiya ◽  
A. A. Amirul ◽  
S. Rizal ◽  
...  
Keyword(s):  
Gamma Irradiation ◽  
Water Solubility ◽  
Composite Films ◽  
Chemical Properties ◽  
Antimicrobial Activities ◽  
Vapour Permeability ◽  
Control Film ◽  
Biocomposite Films ◽  
Neem Leaves ◽  
The Matrix

Neem leaves extract was incorporated into the matrix of seaweed biopolymer, and the seaweed-neem biocomposite films were irradiated with various doses of gamma irradiation (0.5, 1.5, 2.5, 3.5, and 4.5 kGy). The physical, barrier, antimicrobial, and mechanical properties of the films were studied. The incorporation of 5% w/w neem leaves extract into a seaweed-based film, and gamma irradiation dose of 2.5 kGy was most effective for improved properties of the film. The results showed that the interfacial interaction of the seaweed-neem improved with physical changes in colour and opacity. The water solubility, moisture content, and water vapour permeability and biodegradability rate of the film reduced. The contact angle values increased, which was interpreted as improved hydrophobicity. The tensile strength and modulus of the films increased, while the elongation of the composite films decreased compared to the control film. The film’s antimicrobial activities against bacteria were improved. Thus, neem leaves extract in combination with the application of gamma irradiation enhanced the performance properties of the film that has potential as packaging material.

scholarly journals Tissue Interlocking Dissolving Microneedles for Accurate and Efficient Transdermal Delivery of Biomolecules

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Shayan Fakhraei Lahiji ◽  
Youseong Kim ◽  
Geonwoo Kang ◽  
Suyong Kim ◽  
Seunghee Lee ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Dissolving Microneedles

scholarly journals Topical Delivery of Curcumin by Choline-Calix[4]arene-Based Nanohydrogel Improves Its Therapeutic Effect on a Psoriasis Mouse Model

2020 ◽  
Vol 21 (14) ◽  
pp. 5053 ◽  
Author(s):  
Alessia Filippone ◽  
Grazia M. L. Consoli ◽  
Giuseppe Granata ◽  
Giovanna Casili ◽  
Marika Lanza ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Water Solubility ◽  
Skin Diseases ◽  
Local Skin ◽  
Nitric Oxide Synthetase ◽  
Skin Delivery ◽  
Abnormal Distribution ◽  
Tnf Α ◽  
Enhanced Expression ◽  
Inducible Nitric Oxide

Curcumin (CUR) has shown remarkable efficacy in the treatment of skin diseases, but its effective transdermal delivery is still a major challenge and stimulates interest in the design of novel systems for CUR dispersion, preservation, and delivery facilitation to the deeper layers of the skin. The present work aimed to investigate the potential of a nanohydrogel, formed by a micellar choline-calix[4]arene amphiphile (CALIX) and CUR, in the treatment of skin diseases through an imiquimod (IMQ)-induced psoriasis model. Psoriasis plaques are associated with aberrant keratinization, abnormal distribution of tight junctions (TJs) proteins, and enhanced expression of inflammatory markers. The nanohydrogel restored the normal distribution of TJs proteins ZO1 and occludin and reduced the expression of TNF-α and inducible nitric oxide synthetase (iNOS) compared to the untreated IMQ group. The novelty lies in the calix[4]arene-based nanohydrogel as a potential new soft material for the topical skin delivery of CUR. The nanohydrogel, due to its physicochemical and mechanical properties, enhances the drug water-solubility, preserves CUR from rapid degradation, and eases the local skin administration and penetration.

Creep and dynamic mechanical behavior of cross-linked polyvinyl alcohol reinforced with cotton fiber laminate composites

2019 ◽  
Vol 39 (4) ◽  
pp. 326-335 ◽  
Author(s):  
Naman Jain ◽  
Shubhan Ali ◽  
Vinay K. Singh ◽  
Komal Singh ◽  
Nitesh Bisht ◽  
...  
Keyword(s):  
Polyvinyl Alcohol ◽  
Cotton Fiber ◽  
Water Solubility ◽  
Mechanical Analysis ◽  
Cross Linking ◽  
Laminate Composites ◽  
Dynamic Mechanical ◽  
The Matrix ◽  
The Cross ◽  
Uptake Test

AbstractThe objective of this investigation was to fabricate cross-linked polyvinyl alcohol (PVA) based laminate composites reinforced with biaxial cotton sheets. Cross-linking was done with sulfuric acid, to overcome the water solubility of PVA. A water uptake test was performed to evaluate the effect of cross-linking on the water absorption properties of the composites. Morphology, distribution and bonding between the matrix and reinforcement of the fabricated composites were studied using scanning electron microscopy. Mechanical properties such as the tensile strength (TS), modulus of elasticity and elongation of the fabricated composites material were evaluated. There was about a 56.25% increase in the TS of the cross-linked composite as compared to the neat PVA, and at 64 wt.% of cotton fiber, there was about a 56% increase in the TS as compared to the cross-linked PVA. The thermal degradation analysis of fabricated composites material was carried out by thermogravimetric analysis. The thermal stability increased with increase in cotton fiber wt.%. The viscoelastic properties of the fabricated composites material were determined by dynamic mechanical analysis. The effects of stress (4 MPa, 6 MPa and 8 MPa) and temperature (20°C and 40°C) on creep and recovery behavior of the laminated composites were studied.

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