pH-sensitive chitosan nanoparticles loaded with dolutegravir as milk and food admixture for paediatric anti-HIV therapy

Krishnan, Priya Dharshini; Fang, Hao; Devi, D. Ramya; Yang, Jinxuan; Luo, Rong-Hua; Zheng, Yong‐Tang; Brzeziński, Marek; Hari, B.N. Vedha

doi:10.1016/j.carbpol.2020.117440

Cited by 27 publications

(12 citation statements)

References 47 publications

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“…After incubation at room temperature for 1 h, the solution was centrifuged and the supernatant was subjected to UV–Visible spectrophotometry analysis to estimate the amount of drug present in the nanoparticles. The Chitosan nanoparticles showing the maximum drug content of 75 ± 2% were selected as the optimum formulation and results were previously published earlier 19 . Since, spray drying is a process that results in the formation of polymer-drug matrix nanoparticles formed by electrostatic interactions, wherein the drug is expected to present inside and on the surface of the particles, the total drug content in the nanoparticles is estimated instead of encapsulation efficiency.…”

Section: Resultsmentioning

confidence: 99%

“…Enhanced solubility of chitosan-based nanoparticles in acidic pH of the stomach would facilitate the dissolution and bioavailability, which ultimately improve the drug absorption to reach the systemic circulation 20 . The drug release experiments of the nanoparticles were carried out in other media also (distilled water, phosphate buffer pH-6.8, and 0.1 N HCl media in the presence of digestive enzymes like pepsin and pancreatin, and the comparative results were published earlier 19 . The time taken to release 30%, 50%, and 80% (T 30 , T 50, and T 80 , respectively) of the drug from the NPs in the 0.1 N HCl medium was calculated based on the drug release profile.…”

Section: Resultsmentioning

confidence: 99%

“…During the in vitro optimization studies, the Chitosan NPs with the drug and polymer ratio of 1:1 had shown better response in terms of particle size, drug content and drug release rate, etc. 19 . Hence the Rhodamine B dye and the Chitosan polymer were taken in a 1:1 ratio and dissolved in 1% acetic acid and the solution was spray-dried at 140 °C.…”

Section: Methodsmentioning

confidence: 99%

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In-vivo pharmacokinetic studies of Dolutegravir loaded spray dried Chitosan nanoparticles as milk admixture for paediatrics infected with HIV

Banudevi

et al. 2022

Sci Rep

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Dolutegravir (DTG) is an antiretroviral drug approved in the year 2013, and being categorized as a BCS-II molecule, it possesses solubility issues. In order to enhance the solubility and improve its bioavailability, DTG-loaded Chitosan nanoparticles (NPs) were synthesized utilizing spray drying technology. The developed nanoformulation was characterized for its physicochemical properties and investigated for the feasibility of its administration through an oral route along with milk/food as an admixture for paediatric antiretroviral therapy. The in vivo oral bioavailability studies were conducted in Balb-C mice, where the animals were treated with the selected formulation of DTG-loaded Chitosan NPs and compared to pure DTG. The NPs exhibited 2.5-fold increase in the Cmax (77.54 ± 7.93 μg/mL) when compared to the pure DTG (30.15 ± 8.06 μg/mL). This phenomenon was further reflected by the improved bioavailability of DTG (AUC: 678.3 ± 10.07 μg/h/mL) in the NPs administered to mice when compared to the AUC of animals administered with pure DTG (405.29 ± 7 μg/h/mL). Altogether, the research findings showed that Chitosan-based NPs were ideal carriers for oral administration of DTG along with milk and exhibited great potential to enhance the bioavailability of the drug and treatment adherence for paediatric HIV patients.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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In-vivo pharmacokinetic studies of Dolutegravir loaded spray dried Chitosan nanoparticles as milk admixture for paediatrics infected with HIV

Banudevi

et al. 2022

Sci Rep

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“…CS is the only natural polysaccharide with cationic properties and has been widely used in the biomedical, pharmaceutical, cosmetic, and food industries. CS-based vehicles have been recognized as effective drug delivery systems for enhancing the oral bioavailability of drugs, phytochemicals and bioactive macromolecules including proteins, peptides and polysaccharides [ 20 , 21 , 22 , 23 , 24 , 25 , 26 ]. So far, many CS-based drug delivery systems such as hydrogels, microparticles, and nanoparticles (NPs) have been developed [ 20 , 27 , 28 ].…”

Section: Introductionmentioning

confidence: 99%

Biodegradable Nanoparticles Prepared from Chitosan and Casein for Delivery of Bioactive Polysaccharides

et al. 2022

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Ophiopogon japonicus polysaccharides (OJPs) have great anti-inflammation and immunomodulatory abilities. However, the low bioavailability of OJPs reduces its applicability in the biomedical and pharmaceutical fields. Chitosan (CS) has excellent mucoadhesive properties and absorption-enhancing ability in oral administration. Casein hydrolysate (CL) has good interfacial diffusivity and emulsifying ability, and can interact with polysaccharides to form complexes combining the individual properties of both. Therefore, chitosan and casein hydrolysate are good candidates for developing nanoformulations for oral delivery. In this study, bioactive polysaccharides (OJPs), CS and CL, were combined to prepare CS/OJPs/CL co-assembled biodegradable nanoparticles. The interactions between polysaccharides (CS and OJPs) and peptide (CL) resulted in the formation of nanoparticles with an average particle size of 198 nm and high OJPs loading efficiency. The colloidal properties of the nanoparticles were pH-dependent, which were changed significantly in simulated digestive fluid at different pH values. OJPs released from the CS/OJPs/CL nanoparticles were greatly affected by pH and enzymatic degradation (trypsin and lysozyme). The nanoparticles were easily internalized by macrophages, thereby enhancing the OJPs’ inhibitory ability against Ni2+-induced cytotoxicity and LPS-induced nitric oxide production. This study demonstrates that prepared polysaccharide/protein co-assembled nanoparticles can be potential nanocarriers for the oral delivery of bioactive polysaccharides with anti-inflammatory functions.

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“…High ROS levels have been widely used in the development of stimulus-responsive drug delivery systems. Compared with widely used intrinsic signals such as pH and GSH, ROS in tumor tissues has higher speci city [17][18][19][20].…”

Section: Introductionmentioning

confidence: 99%

Novel ROS-responsive marine biomaterial fucoidan nanocarriers with AIE effect and chemodynamic therapy

Guo

Cheng

et al. 2022

International Journal of Biological Macromolecules

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Chemodynamic therapy (CDT) has been widely used in the treatment of many kinds of tumors, which can effectively induce tumor cell apoptosis by using produced reactive oxygen species (ROS). In this paper, ROS-sensitive multifunctional marine biomaterial natural polysaccharide nanoparticles (CT/PTX) were designed. Aggregation-induced emission (AIE) molecules tetraphenylethylene (TPE) labeled and caffeic acid (CA) modi ed fucoidan (FUC) amphiphilic carrier material (CA-FUC-TK-TPE, CFTT) was fabricated, in which the thioketal bond was used as the linkage arm between TPE and fucoidan chain, giving the CFTT material ROS sensitivity. In addition, amphiphilic carrier material (FUC-TK-VE, FTVE) composed of thioketal-linked vitamin E and fucoidan was synthesized. The mixed carrier material CFTT and FTVE selfassembled in water to form nanoparticles (CT/PTX ) loaded with PTX and Fe 3+ . CT/PTX nanoparticles could induce ROS oxidative stress in tumor sites through the CDT effect induced by Fe 3+ . The CDT effect was combined with the chemotherapeutic drug PTX to achieve tumor inhibition. In vitro cell studies have proved that CT/PTX nanoparticles have excellent cell permeability and tumor cytotoxicity. In vivo antitumor experiments con rmed effective antitumor activity and reduced side effects.

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pH-sensitive chitosan nanoparticles loaded with dolutegravir as milk and food admixture for paediatric anti-HIV therapy

Cited by 27 publications

References 47 publications

In-vivo pharmacokinetic studies of Dolutegravir loaded spray dried Chitosan nanoparticles as milk admixture for paediatrics infected with HIV

In-vivo pharmacokinetic studies of Dolutegravir loaded spray dried Chitosan nanoparticles as milk admixture for paediatrics infected with HIV

Biodegradable Nanoparticles Prepared from Chitosan and Casein for Delivery of Bioactive Polysaccharides

Novel ROS-responsive marine biomaterial fucoidan nanocarriers with AIE effect and chemodynamic therapy

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