Covalent Conjugation of Amphotericin B to Hyaluronic Acid: An Injectable Water-Soluble Conjugate with Reduced Toxicity and Anti-Leishmanial Potential

2022 ◽  
Author(s):  
Ricardo Silva-Carvalho ◽  
Teresa Leão ◽  
Francisco M. Gama ◽  
Ana M. Tomás
Keyword(s):  
Hyaluronic Acid ◽  
Amphotericin B ◽  
Water Soluble ◽  
Reduced Toxicity

scholarly journals Wound Healing Promotion by Hyaluronic Acid: Effect of Molecular Weight on Gene Expression and In Vivo Wound Closure

2021 ◽  
Vol 14 (4) ◽  
pp. 301
Author(s):  
Yayoi Kawano ◽  
Viorica Patrulea ◽  
Emmanuelle Sublet ◽  
Gerrit Borchard ◽  
Takuya Iyoda ◽  
...  
Keyword(s):  
Gene Expression ◽  
Molecular Weight ◽  
Wound Healing ◽  
Hyaluronic Acid ◽  
Healing Process ◽  
Dermal Fibroblasts ◽  
Water Soluble ◽  
Wound Healing Process ◽  
And Migration ◽  
Proliferation And Migration

Hyaluronic acid (HA) has been known to play an important role in wound healing process. However, the effect of molecular weight (MW) of exogenously administered HA on the wound healing process has not been fully understood. In this study, we investigated HA with different MWs on wound healing process using human epidermal keratinocytes and dermal fibroblasts. Cell proliferation and migration ability were assessed by water soluble tetrazolium (WST) assay and wound scratch assay. We examined the effect of HA addition in a full-thickness wound model in mice and the gene expression related to wound healing. Proliferation and migration of HaCaT cells increased with the increase of MW and concentration of HA. Interleukin (IL-1β), IL-8 and vascular endothelial growth factor (VEGF) as well as matrix metalloproteinase (MMP)-9 and MMP-13 were significantly upregulated by high molecular weight (HMW) HA in keratinocytes. Together with VEGF upregulation and the observed promotion of HaCaT migration, HA with the MW of 2290 kDa may hold potential to improve re-epithelialization, a critical obstacle to heal chronic wounds.

Preparation of cross-linked hyaluronic acid film using 2-chloro-1-methylpyridinium iodide or water-soluble 1-ethyl-(3,3-dimethylaminopropyl)carbodiimide

2004 ◽  
Vol 15 (6) ◽  
pp. 767-780 ◽  
Author(s):  
Jenn-Jong Young ◽  
Kuang-Ming Cheng ◽  
Tai-Li Tsou ◽  
Hwan-Wun Liu ◽  
Hsian-Jenn Wang
Keyword(s):  
Hyaluronic Acid ◽  
Water Soluble

scholarly journals Water-Soluble Blue Fluorescent Nonconjugated Polymer Dots from Hyaluronic Acid and Hydrophobic Amino Acids

ACS Omega ◽  
2021 ◽  
Author(s):  
Deep S. Bhattacharya ◽  
Aishwarya Bapat ◽  
Denis Svechkarev ◽  
Aaron M. Mohs
Keyword(s):  
Amino Acids ◽  
Hyaluronic Acid ◽  
Water Soluble ◽  
Polymer Dots ◽  
Hydrophobic Amino Acids

scholarly journals ENHANCEMENT OF THE SOLUBILITY OF FAMOTIDINE SOLID DISPERSION USING NATURAL POLYMER BY SOLVENT EVAPORATION

2021 ◽  
pp. 193-198
Author(s):  
HUSSEIN K. ALKUFI ◽  
ASMAA M. RASHID
Keyword(s):  
Hyaluronic Acid ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Natural Polymer ◽  
Solubility Study ◽  
Poorly Soluble ◽  
Pure Drug

Objective: The aims of the study to enhance solubility and dissolution of famotidine using natural polymer. Solubility study of a drug is one of the contributing factors of its oral bioavailability. The formulation of poorly soluble drugs for oral delivery presents a challenge to the formulation technologists. Methods: The present study has shown that it is possible to raise the solubility for poorly soluble drugs like famotidine, by preparing solid dispersion using natural water-soluble polymer (xyloglucan and hyaluronic acid) as solubilizer through solvent evaporation method. Physical mixture and solid dispersion of famotidine with xyloglucan (XG) or hyaluronic acid in a ratio of 1:1, 1:2, 1:3 were prepared. Solubility study, drug content, dissolution profile and compatibility study were performed for famotidine in solid dispersions XS1, XS2, XS3, HS4, HS5, HS6 as well as in physical mixtures at a ratio 1:1 for both polymer (XG and hyaluronic acid). Results: It was observed that solid dispersions of each drugs showed an increase in dissolution rate in comparison with its pure drug in the ratio of 1:1 (Drug: carrier). It can be concluded that with the care and proper use of xyloglucan, the solubility of drugs poorly soluble can be improved. The prepared solid dispersion showed improvement of drug solubility in all prepared formulas. The best result was obtained with formula XS1 (famotidine: xyloglucan at ratio 1:1) that showed 26 fold increase in solubility compared to the solubility of pure drug. Conclusion: The natural solid dispersion, increased wettability and reduced crystallinity of the drug which leads to improving solubility and dissolution.

Europium(III)-induced water-soluble nano-aggregates of hyaluronic acid and chitosan: structure and fluorescence

2018 ◽  
Vol 8 (03) ◽  
pp. 1224-1229 ◽  
Author(s):  
Junlan Guo ◽  
Jianguo Tang ◽  
Jing Wang ◽  
Sui Mao ◽  
Haidong Li ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Water Soluble ◽  
Image Position

Abstract

scholarly journals Encochleated Amphotericin B: Is the Oral Availability of Amphotericin B Finally Reached?

2020 ◽  
Vol 6 (2) ◽  
pp. 66
Author(s):  
Maria Aigner ◽  
Cornelia Lass-Flörl
Keyword(s):  
Amphotericin B ◽  
The Novel ◽  
Phase Ii Clinical Trials ◽  
Wide Range ◽  
Life Threatening ◽  
Oral Availability ◽  
Reduced Toxicity ◽  
Yeasts And Molds ◽  
Lipid Formulations ◽  
Cargo Molecule

As the oldest and for many decades the only available agent for the treatment of life-threatening invasive fungal diseases, amphotericin B (AmB) is known for its broad-spectrum fungicidal activity against a wide range of yeasts and molds. However, the main drawback of the present formulations remains its toxicity, the limited use to intravenous administration, and the higher costs associated with the better tolerated lipid formulations. The novel nanoparticle-based encochleated AmB (CAmB) formulation encapsulates, protects, and delivers its cargo molecule AmB in the interior of a calcium-phospholipid anhydrous crystal. Protecting AmB from harsh environmental conditions and gastrointestinal degradation, CAmB offers oral availability in conjunction with reduced toxicity. Matinas BioPharma, Bedminster, NJ is on the way to develop CAmB named MAT2203, currently undergoing Phase II clinical trials.

A Novel Water-Soluble Heptaplatin Analogue with Improved Antitumor Activity and Reduced Toxicity

2011 ◽  
Vol 50 (12) ◽  
pp. 5324-5326 ◽  
Author(s):  
Weiping Liu ◽  
Xizhu Chen ◽  
Qingsong Ye ◽  
Yongping Xu ◽  
Chengying Xie ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Reduced Toxicity

scholarly journals Amphotericin B-conjugated polypeptide hydrogels as a novel innovative strategy for fungal infections

2018 ◽  
Vol 5 (3) ◽  
pp. 171814 ◽  
Author(s):  
Chang Shu ◽  
Tengfei Li ◽  
Wen Yang ◽  
Duo Li ◽  
Shunli Ji ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Antifungal Activity ◽  
Amphotericin B ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
Water Soluble ◽  
Naphthalene Acetic Acid ◽  
Innovative Strategy ◽  
Molecular Arrangement

The present work is focused on the design and development of novel amphotericin B (AmB)-conjugated biocompatible and biodegradable polypeptide hydrogels to improve the antifungal activity. Using three kinds of promoting self-assembly groups (2-naphthalene acetic acid (Nap), naproxen (Npx) and dexamethasone (Dex)) and polypeptide sequence (Phe-Phe-Asp-Lys-Tyr, FFDKY), we successfully synthesized the Nap-FFDK(AmB)Y gels, Npx-FFDK(AmB)Y gels and Dex-FFDK(AmB)Y gels. The AmB-conjugated hydrogelators are highly soluble in different aqueous solutions. The cryo-transmission electron microscopy and scanning electron microscopy micrographs of hydrogels afford nanofibres with a width of 20–50 nm. Powder X-ray diffraction analyses demonstrate that the crystalline structures of the AmB and Dex are changed into amorphous structures after the formation of hydrogels. Circular dichroism spectra of the solution of blank carriers and the corresponding drug deliveries further help elucidate the molecular arrangement in gel phase, indicating the existence of turn features. The in vitro drug releases suggest that the AmB-conjugated hydrogels are suitable as drug-controlled release vehicles for hydrophobic drugs. The antifungal effect of AmB-conjugated hydrogels significantly exhibits the antifungal activity against Candida albicans . The results of the present study indicated that the AmB-conjugated hydrogels are suitable carriers for poorly water soluble drugs and for enhancement of therapeutic efficacy of antifungal drugs.

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