Development of Biodegradable Delivery Systems Containing Novel 1,2,4-Trioxolane Based on Bacterial Polyhydroxyalkanoates

Lipaikin, S.Y.; Yaremenko, Ivan A.; Terent’ev, Alexander O.; Volova, Tatiana G.; Shishatskaya, Ekaterina I.

doi:10.1155/2022/6353909

Cited by 4 publications

(4 citation statements)

References 70 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…We have previously shown that PHA microparticles and films containing synthetic ozonide peroxide (OZ) inhibit cell growth and proliferation. The viability of HeLa cells when adding OZ-containing samples was 2-10%, compared to the control group (blank films and microparticles prepared from P3HB and P3HB/3HV), where the cell viability was at the level of 90% [104]. On the whole, in a culture of HeLa cells, the cytostatic efficacy of the 5-fluorouracil loaded in PHAs microparticles is shown.…”

Section: Antibacterial and Antitumor Efficacy Of Drug-loaded Pha Micr...mentioning

confidence: 87%

Characteristics of Microparticles Based on Resorbable Polyhydroxyalkanoates Loaded with Antibacterial and Cytostatic Drugs

Murueva,

Shershneva,

Shishatskaya

et al. 2023

IJMS

Self Cite

View full text Add to dashboard Cite

The development of controlled drug delivery systems, in the form of microparticles, is an important area of experimental pharmacology. The success of the design and the quality of the obtained microparticles are determined by the method of manufacture and the properties of the material used as a carrier. The goal is to obtain and characterize microparticles depending on their method of preparation, the chemical composition of the polymer and the load of the drugs. To obtain microparticles, four types of degradable PHAs, differing in their chemical compositions, degrees of crystallinity, molecular weights and temperature characteristics, were used (poly-3-hydroxybutyrate and copolymers 3-hydroxybutyric-co-3-hydroxyvaleric acid, 3-hydroxybutyric-co-4-hydroxybutyric acid, and 3-hydroxybutyric-co-3-hydroxyhexanoic acid). The characteristics of microparticles from PHAs were studied. Good-quality particles with an average particle diameter from 0.8 to 65.0 μm, having satisfactory ζ potential values (from −18 to −50 mV), were obtained. The drug loading content, encapsulation efficiency and in vitro release were characterized. Composite microparticles based on PHAs with additives of polyethylene glycol and polylactide-co-glycolide, and loaded with ceftriaxone and 5-fluorouracil, showed antibacterial and antitumor effects in E. coli and HeLa cultures. The results indicate the high potential of PHAs for the design of modern and efficient drug delivery systems.

show abstract

Section: Antibacterial and Antitumor Efficacy Of Drug-loaded Pha Micr...mentioning

confidence: 87%

Characteristics of Microparticles Based on Resorbable Polyhydroxyalkanoates Loaded with Antibacterial and Cytostatic Drugs

Murueva,

Shershneva,

Shishatskaya

et al. 2023

IJMS

Self Cite

View full text Add to dashboard Cite

show abstract

“…Vennerstrom et al reported in 2008 that OZ277 generated the ineffectual OZ381 173a and OZ397 173b carbinol metabolites (IC 50 = 10 −6 mol/L against the P. falciparum strain CQ‐resistant K1) to hydrolysis by human liver microsome, of 4a (OZ277, IC 50 = 2.54 × 10 −9 mol/L) 232,233 . It has been found that ozonides OZ277 and OZ418 are able to inhibit α‐coronavirus NL63, β‐coronavirus OC43, and SARC‐CoV‐2 234 . Extensive research also revealed that the spiroadamantane ring on the final staging point was hydroxylated.…”

Section: Some Antimalarial Endoperoxide Moieties Other Than 124‐triox...mentioning

confidence: 99%

“…232,233 It has been found that ozonides OZ277 and OZ418 are able to inhibit α-coronavirus NL63, β-coronavirus OC43, and SARC-CoV-2. 234 Extensive research also revealed that the spiroadamantane ring on the final staging point was hydroxylated. As a result of the same sterically compromised composition of such ozone products, the spiroadamantane chain is unable to react with Fe (II) within parasites, preventing their medicinal effect.…”

Section: Trioxolane-polyamine Conjugatesmentioning

confidence: 99%

An overview on the antimalarial activity of 1,2,4‐trioxanes, 1,2,4‐trioxolanes and 1,2,4,5‐tetraoxanes

Shukla

Rathi

Hassam³

et al. 2023

Medicinal Research Reviews

View full text Add to dashboard Cite

The demand for novel, fast‐acting, and effective antimalarial medications is increasing exponentially. Multidrug resistant forms of malarial parasites, which are rapidly spreading, pose a serious threat to global health. Drug resistance has been addressed using a variety of strategies, such as targeted therapies, the hybrid drug idea, the development of advanced analogues of pre‐existing drugs, and the hybrid model of resistant strains control mechanisms. Additionally, the demand for discovering new potent drugs grows due to the prolonged life cycle of conventional therapy brought on by the emergence of resistant strains and ongoing changes in existing therapies. The 1,2,4‐trioxane ring system in artemisinin (ART) is the most significant endoperoxide structural scaffold and is thought to be the key pharmacophoric moiety required for the pharmacodynamic potential of endoperoxide‐based antimalarials. Several derivatives of artemisinin have also been found as potential treatments for multidrug‐resistant strain in this area. Many 1,2,4‐trioxanes, 1,2,4‐trioxolanes, and 1,2,4,5‐tetraoxanes derivatives have been synthesised as a result, and many of these have shown promise antimalarial activity both in vivo and in vitro against Plasmodium parasites. As a consequence, efforts to develop a functionally straight‐forward, less expensive, and vastly more effective synthetic pathway to trioxanes continue. This study aims to give a thorough examination of the biological properties and mode of action of endoperoxide compounds derived from 1,2,4‐trioxane‐based functional scaffolds. The present system of 1,2,4‐trioxane, 1,2,4‐trioxolane, and 1,2,4,5‐tetraoxane compounds and dimers with potentially antimalarial activity will be highlighted in this systematic review (January 1963–December 2022).

show abstract

“…The uniqueness of this class of materials is that it is possible to obtain copolymers of various compositions with different physical and mechanical properties. It is known that the inclusion of such monomers as 4-hydroxybutyrate (4HB), 3-hydroxyvalerate (3HV), and 3-hydroxyhexanoate (3HHx) affects the physical and mechanical properties [ 47 , 48 , 49 ]. Features of the microstructure and surface relief of PHA samples of different monomeric composition depend on the inclusion of these monomers, which affect the biological properties [ 50 , 51 ].…”

Section: Introductionmentioning

confidence: 99%

Influence of PHA Substrate Surface Characteristics on the Functional State of Endothelial Cells

Ryltseva

Dudaev

Menzyanova

et al. 2023

JFB

Self Cite

View full text Add to dashboard Cite

The needs of modern regenerative medicine for biodegradable polymers are wide and varied. Restoration of the viability of the vascular tree is one of the most important components of the preservation of the usefulness of organs and tissues. The creation of vascular implants compatible with blood is an important task of vascular bioengineering. The function of the endothelial layer of the vessel, being largely responsible for the development of thrombotic complications, is of great importance for hemocompatibility. The development of surfaces with specific characteristics of biomaterials that are used in vascular technologies is one of the solutions for their correct endothelialization. Linear polyhydroxyalkanoates (PHAs) are biodegradable structural polymeric materials suitable for obtaining various types of implants and tissue engineering, having a wide range of structural and physicomechanical properties. The use of PHA of various monomeric compositions in endothelial cultivation makes it possible to evaluate the influence of material properties, especially surface characteristics, on the functional state of cells. It has been established that PHA samples with the inclusion of 3-hydroxyhexanoate have optimal characteristics for the formation of a human umbilical vein endothelial cell, HUVEC, monolayer in terms of cell morphology as well as the levels of expression of vinculin and VE-cadherin. The obtained results provide a rationale for the use of PHA copolymers as materials for direct contact with the endothelium in vascular implants.

show abstract

Development of Biodegradable Delivery Systems Containing Novel 1,2,4-Trioxolane Based on Bacterial Polyhydroxyalkanoates

Cited by 4 publications

References 70 publications

Characteristics of Microparticles Based on Resorbable Polyhydroxyalkanoates Loaded with Antibacterial and Cytostatic Drugs

Characteristics of Microparticles Based on Resorbable Polyhydroxyalkanoates Loaded with Antibacterial and Cytostatic Drugs

An overview on the antimalarial activity of 1,2,4‐trioxanes, 1,2,4‐trioxolanes and 1,2,4,5‐tetraoxanes

Influence of PHA Substrate Surface Characteristics on the Functional State of Endothelial Cells

Contact Info

Product

Resources

About