Delving into the Latest Updates on Hyaluronic acid/Fluorouracil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

HA-5-fluorouracil, Hyaluronan acid-5-fluorouracil complex, Hyaluronic acid-5-fluorouracil complex

+ [2]

Target

CD44 x TYMS

Mechanism

CD44 modulators(CD44 antigen modulators), TYMS inhibitors(Thymidylate synthase inhibitors)

Therapeutic Areas

NeoplasmsDigestive System Disorders

Active Indication

Colorectal Cancer

Inactive Indication-

Originator Organization

Monash University

Active Organization

Alchemia Oncology Pty Ltd.

Monash University

Inactive Organization

The Sustainable Nutrition Group Pty Ltd.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC4H3FN2O2

InChIKeyGHASVSINZRGABV-UHFFFAOYSA-N

CAS Registry51-21-8

PurposeThere is growing interest in combining topical treatments with aesthetic procedures to combat signs of aging skin. This study aimed to assess the efficacy and tolerability of a novel cosmetic serum containing 5 different forms of HA (HA⁵ DG) when used via a proprietary diamond-tip microdermabrasion procedure (DG) to treat skin dryness, fine lines/wrinkles, rough texture, and dullness.Patients and MethodsIn this open-label, single-center study, participants received HA⁵ DG as part of a biweekly DG procedure on the face and neck for 12 weeks. Study participants also applied another take-home HA⁵ serum to the face twice daily at home, along with a basic skincare regimen. The efficacy of the combined treatment was measured by clinical quantification of multiple skin appearance features, analysis of bioinstrumental measurements, and digital photography.ResultsThis study enrolled 27 participants, with an average age of 42.7 years and Fitzpatrick skin phototypes I-III (59.3%), IV (18.5%), and V-VI (22.2%), and 23 participants completed the study. The combined treatment had effects in fine lines/wrinkles, skin dryness, smoothness, radiance, firmness, and hydration 15 minutes post-DG. Furthermore, the significant improvements observed in dryness, fine lines/wrinkles, skin smoothness, and radiance were still visible 3 days after and maintained at week 12. Additionally, smoothing of coarse lines/wrinkles, improvement of skin tone evenness, hyperpigmentation, photodamage, and transepidermal water loss were observed at week 12. The treatment had a favorable tolerability profile and was perceived as efficacious and highly satisfactory.ConclusionThis novel combined treatment delivered immediate and prolonged skin hydration and high participant satisfaction, proving it can be an excellent approach for skin rejuvenation.

01 Dec 2022·International Journal of Biological Macromolecules

Effects of the molecular weight of hyaluronan on the conformation and release kinetics of self-assembled 5-fluorouracil-loaded lysozyme-hyaluronan colloidal nanoparticles

Article

Author: Zhang, Xin ; Wu, Songgu ; Li, Maolin ; Wei, Jiahao ; Han, Dandan ; Gong, Junbo ; Liu, Yanbo

Lysozyme (LYS) and hyaluronan with low (HA1: 3 kDa), medium (HA2: 120 kDa), and high (HA3: 1200 kDa) molecular weights were used to fabricate lysozyme-hyaluronan colloidal nanoparticles using a green self-assembly method. Fourier transform infrared spectroscopy indicated that hydrogen bonding, hydrophobic and electrostatic interactions promoted the formation of the colloidal nanoparticles. The hydrophobic area of prepared colloidal nanoparticles was quantified using a pyrene fluorescent probe, and the results showed that the LYS-HA3 nanoparticles had the strongest hydrophobic capacity. Furthermore, 5-fluorouracil (5-Fu) was used to evaluate encapsulation performance, demonstrating that the LYS-HA3 nanoparticles had the highest encapsulation ability (>90 %). All prepared 5-Fu-loaded lysozyme-hyaluronan (5-Fu@LYS-HA) colloidal nanoparticles exhibited excellent long-term storage stability at 4 °C for 60 days. Cellular uptake and in vitro release results indicated that the LYS-HA2 nanoparticles exhibited the highest cellular uptake efficiency, and the LYS-HA3 nanoparticles had the best slow-release effect, while the release process was mainly controlled by the combination of Fickian diffusion and structural relaxation, respectively. This study demonstrates the influence of molecular weight on the conformational and structural properties of colloidal nanoparticles, which has implications for the design of insoluble drug self-assembly systems.

01 Oct 2020·Journal of Cellular PhysiologyQ2 · BIOLOGY

Hyaluronic acid‐decorated liposomal nanoparticles for targeted delivery of 5‐fluorouracil into HT‐29 colorectal cancer cells

Q2 · BIOLOGY

Article

Author: Abedi‐Gaballu, Fereydoon ; Dehghan, Gholamreza ; Mansoori, Behzad ; Baradaran, Behzad ; Yekta, Reza ; Abbaspour, Soheil ; Ghasabi, Mehri ; Hamblin, Michael R. ; Shirjang, Solmaz ; Mohammadi, Ali

AbstractThe use of liposomes as drug carriers improves the therapeutic efficacy of anticancer drugs, while at the same time reducing side effects. Hyaluronic acid (HA) is recognized by the CD44 receptor, which is overexpressed in many cancer cells. In this study, we developed HA‐modified liposomes encapsulating 5‐fluorouracil (5‐FU) and tested them against a CD44 expressing colorectal cell line (HT29) and a non‐CD44 expressing hepatoma cell line. The average size of 5‐FU‐lipo and 5‐FU‐lipo‐HA nanoparticles were 112 ± 28 and 144 ± 77 nm, respectively. The 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium (MTT) assay showed selective cancer cell death depending on the CD44 expression in a time‐dependent manner. Apoptosis assays and cell‐cycle analysis indicated that G0/G1 arrest occurred. The colony formation study revealed that cells treated with 5‐FU‐lipo and 5‐FU‐lipo‐HA had reduced colony formation. Quantitative reverse‐transcription polymerase chain reaction study showed that the oncogenic messenger RNA and microRNA levels were significantly reduced in the 5‐FU‐lipo‐HA‐treated group, while tumor suppressors were increased in that group. We suggest that optimal targeted delivery and release of 5‐FU into colorectal cancer cells, renders them susceptible to apoptosis, cell‐cycle arrest, and decreased colony formation.

100 Deals associated with Hyaluronic acid/Fluorouracil

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Colorectal Cancer	Phase 2	-	Alchemia Oncology Pty Ltd.	-
Colorectal Cancer	Phase 2	-	Monash University	-
Colorectal Cancer	Discovery	AU	The Sustainable Nutrition Group Pty Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00682786 (CTgov)	Phase 2	Rectal Cancer	135	Radiation+5FU (Good Risk (Thymidylate Synthase (TYMS)2/2, 2/3, 2/4))	pzptvicgmq(qtfdytevdz) = pkbkmtegpy ivrkxswgdo (lgignuvgna, fsmcjmdhdp - cppjyytfrf) View more	-	08 Sep 2014
NCT00682786 (CTgov)	Phase 2	Rectal Cancer	135	Radiation+5FU+Irinotecan (Poor Risk (Thymidylate Synthase (TYMS)3/3, 3/4))	pzptvicgmq(qtfdytevdz) = abpmudlfsl ivrkxswgdo (lgignuvgna, rjgpgtyjcl - jsjquxpwhf) View more	-	08 Sep 2014
ASCO2012	Phase 1	Liver metastases	19	HA FUDR	rexgkuwkxg(ayiendlcch) = fnihoyefsb xjljngapbo (agrhgpuwyf ) View more	-	20 May 2012
NCT00463840 (CTgov)	Phase 1/2	Locally Advanced Pancreatic Adenocarcinoma	24	FOLFOX 6+5FU+oxaliplatin	ajmpvzeiio(dodkgtehqc) = qosdrhrqqf psgstfifmh (uxcnhhwjcz, hbutcgobxr - xtcldaagsg) View more	-	01 May 2012