Preparation and application of micro/nanoparticles based on natural polysaccharides

Yang, Jisheng; Han, Suya; Zheng, Haicheng; Dong, Hanshan; Liu, Jiubing

doi:10.1016/j.carbpol.2015.01.029

Cited by 232 publications

(112 citation statements)

References 175 publications

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“…Dextran nanoparticle-based drug delivery systems are biocompatible and biodegradable, possess low immunogenicity (19), and can be used for controlled release of pharmacologically active substances (26). We therefore encapsulated optically enriched Novel Optically Enriched Fluconazole Analogues Antimicrobial Agents and Chemotherapy nanoparticles were 50% Ϯ 4%, 22% Ϯ 2%, and 30% Ϯ 2%, respectively), the resulting particle size distributions were determined using dynamic light scattering (DLS).…”

Section: Resultsmentioning

confidence: 99%

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Chemoenzymatic Synthesis, Nanotization, and Anti-Aspergillus Activity of Optically Enriched Fluconazole Analogues

Malhotra

Singh

Rana

et al. 2017

Antimicrob Agents Chemother

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Despite recent advances in diagnostic and therapeutic methods in antifungal research, aspergillosis still remains a leading cause of morbidity and mortality. One strategy to address this problem is to enhance the activity spectrum of known antifungals, and we now report the first successful application of Candida antarctica lipase (CAL) for the preparation of optically enriched fluconazole analogues. AntiAspergillus activity was observed for an optically enriched derivative, (Ϫ)-S-2-(2=,4=-difluorophenyl)-1-hexyl-amino-3-(1ٞ,2ٞ,4ٞ)triazol-1ٞ-yl-propan-2-ol, which exhibits MIC values of 15.6 g/ml and 7.8 g/disc in broth microdilution and disc diffusion assays, respectively. This compound is tolerated by mammalian erythrocytes and cell lines (A549 and U87) at concentrations of up to 1,000 g/ml. When incorporated into dextran nanoparticles, the novel, optically enriched fluconazole analogue exhibited improved antifungal activity against Aspergillus fumigatus (MIC, 1.63 g/ml).These results not only demonstrate the ability of biocatalytic approaches to yield novel, optically enriched fluconazole derivatives but also suggest that enantiomerically pure fluconazole derivatives, and their nanotized counterparts, exhibiting antiAspergillus activity may have reduced toxicity. KEYWORDS chemoenzymatic synthesis, fluconazole, antifungal agents, AspergillusA spergillosis remains a significant threat to public health, and in spite of continuous efforts to improve timely diagnosis and clinical therapies, mortality caused by this disease remains unacceptably high (1, 2). Current therapeutic options for treating Aspergillus-induced disorders include antifungal agents such as polyenes, azoles, and echinocandins (3, 4). Thus, the discovery of new antifungal compounds remains important given the need to address the development of drug resistance in pathogenic fungi (5-7). One approach to accomplishing this goal is to prepare new derivatives of existing drugs with broad-spectrum activity and enhanced pharmacokinetic properties. As part of our ongoing efforts to use lipases (8-12), which catalyze reactions with high degrees of chemo-, regio-, and stereoselectivity in organic synthesis, we became interested in preparing new antifungals using biocatalysis.Fluconazole, introduced in 1990, is a bis-triazole antifungal drug which possesses

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Section: Resultsmentioning

confidence: 99%

“…In vitro assays show that the optically enriched analogues exhibit more potent antifungal activity than the corresponding racemic mixtures. Interestingly, this bioactivity can be enhanced by their encapsulation in dextran-based nanoparticles (19).…”

mentioning

confidence: 99%

Chemoenzymatic Synthesis, Nanotization, and Anti-Aspergillus Activity of Optically Enriched Fluconazole Analogues

Malhotra

Singh

Rana

et al. 2017

Antimicrob Agents Chemother

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“…Pharmacokinetics studies of drug‐conjugated polysaccharides have demonstrated the advantage of using the natural polymers. Although synthetic, water‐soluble polymers have been widely utilized, natural polymers such as chitosan, dextran, cellulose, and hyaluronic acid are also used because of their remarkable potential as drug carriers . For example, doxorubicin (DOX) prodrug nanoparticles with pH‐sensitive drug release properties and antitumor activity were designed and synthesized by conjugating the hydrophobic DOX with chitosan through an acid‐cleavable hydrazone (hz) bond .…”

Section: Polysaccharide–drug Conjugatesmentioning

confidence: 99%

Biodegradable Polysaccharides for Controlled Drug Delivery

et al. 2016

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Polysaccharides are ideal candidates for drug delivery and biomedical applications as they are easily obtained from natural sources. Furthermore, they can be subjected to a wide range of chemical and enzymatic reactions, they have biocompatible and biodegradable properties and have inherently low immunogenicity. Polysaccharides are potentially the materials of choice for the development of “smart” delivery systems, which are capable of releasing, at the appropriate time and site of action, an encapsulated drug. This Review examines various aspects of the crosslinking of polysaccharides, either for a single polysaccharide or mixtures, and also natural–synthetic hybrids. The Review focuses on the strategies for using these biodegradable polymers for controlled drug delivery, and examines in particular polysaccharide–drug conjugates, the encapsulation of drugs in hydrogels and aerogels, and the self‐assembly of polysaccharide drug‐loaded nanoparticles.

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“…In humans, the equivalent pore diameter has been estimated to be between 4 and 8 Ȧ and about 10-15 Ȧ in rat and rabbit. The mucosal epithelium in the small intestine consists of polarized cells, connected by tight intercellular junctions, which account for < 1% of the surface area of the intestine 15 . Fig.…”

Section: Channels Of Uptakementioning

confidence: 99%

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2017

IJPSR

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Peptide drugs are poorly absorbable and are also susceptible to enzymatic degradation in the gastrointestinal tract (GIT). To overcome the physiological and morphological barriers for the peptide / poorly absorbable drug delivery, mucopenetrative and mucoadhesive properties of drug carriers have to be considered. Mucoadhesion can prolong the residence time of drug carriers at the absorption sites, improved drug absorption and controlled release of drug from the device used. The particles with smaller size were likely to diffuse much faster into the mucus layer, provided that diffusion of the particles into the mucus layer should obey Stokes-Einstein equation. The adhesiveness of the nanoparticles (NPs) in suspension form helps to improve bioavailability. Chitosan (CS) based or CS-coated NPs represent another common group of mucoadhesive systems. Moreover, NPs made of such polymers were used to enhance the bioavailability, and also the mucoadhesion of proteins, peptides and DNA to the mucosal tissues. This review focuses on the mechanism of gastrointestinal mucoadhesion of NPs for peptide/poorly absorbable drugs.

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Preparation and application of micro/nanoparticles based on natural polysaccharides

Cited by 232 publications

References 175 publications

Chemoenzymatic Synthesis, Nanotization, and Anti-Aspergillus Activity of Optically Enriched Fluconazole Analogues

Chemoenzymatic Synthesis, Nanotization, and Anti-Aspergillus Activity of Optically Enriched Fluconazole Analogues

Biodegradable Polysaccharides for Controlled Drug Delivery

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