Chitosan nanoparticles for the oral delivery of tenofovir disoproxil fumarate: formulation optimization, characterization and <i>ex vivo</i> and <i>in vivo</i> evaluation for uptake mechanism in rats

Shailender, Joseph; Ravi, Punna Rao; Sirukuri, Mrinalini Reddy; Dalvi, Avantika; Priya, Odapalli Keerthi

doi:10.1080/03639045.2018.1438459

Cited by 28 publications

(13 citation statements)

References 45 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Ulu et al aimed to develop TAF loaded in simple chitosan nanoparticles and found an EE of approximately 50% [ 29 ]. In another study, Shailender et al found an EE of 48.2%, but they prepared nanoparticles of chitosan loaded with a drug that was similar to that used in the current project [ 35 ]. The literature reported the effect of the molecular weight of the polymer and found that the EE and molecular weight have a direct relation with each other [ 36 ].…”

Section: Resultsmentioning

confidence: 99%

“…The results were similar to the study reported by Ulu et al, where a higher zeta potential of 42.8 mV was observed for chitosan due to its cationic nature [ 29 , 41 ]. In other studies, Yien et al [ 42 ] and Shailender et al [ 35 ] prepared drug-loaded chitosan nanoparticles and reported higher zeta potential values. Similar results were reported by Machado et al, where they fabricated composites of nanoparticles (tenofovir-loaded poly(lactic-co-glycolic acid)/stearylamine) [ 43 ].…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Fabrication of PEGylated Chitosan Nanoparticles Containing Tenofovir Alafenamide: Synthesis and Characterization

et al. 2022

View full text Add to dashboard Cite

Tenofovir alafenamide (TAF) is an antiretroviral (ARV) drug that is used for the management and prevention of human immunodeficiency virus (HIV). The clinical availability of ARV delivery systems that provide long-lasting protection against HIV transmission is lacking. There is a dire need to formulate nanocarrier systems that can help in revolutionizing the way to fight against HIV/AIDS. Here, we aimed to synthesize a polymer using chitosan and polyethylene glycol (PEG) by the PEGylation of chitosan at the hydroxyl group. After successful modification and confirmation by FTIR, XRD, and SEM, TAF-loaded PEGylated chitosan nanoparticles were prepared and analyzed for their particle size, zeta potential, morphology, crystallinity, chemical interactions, entrapment efficacy, drug loading, in vitro drug release, and release kinetic modeling. The fabricated nanoparticles were found to be in a nanosized range (219.6 nm), with ~90% entrapment efficacy, ~14% drug loading, and a spherical uniform distribution. The FTIR analysis confirmed the successful synthesis of PEGylated chitosan and nanoparticles. The in vitro analysis showed ~60% of the drug was released from the PEGylated polymeric reservoir system within 48 h at pH 7.4. The drug release kinetics were depicted by the Korsmeyer–Peppas release model with thermodynamically nonspontaneous drug release. Conclusively, PEGylated chitosan has the potential to deliver TAF from a nanocarrier system, and in the future, cytotoxicity and in vivo studies can be performed to further authenticate the synthesized polymer.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Fabrication of PEGylated Chitosan Nanoparticles Containing Tenofovir Alafenamide: Synthesis and Characterization

et al. 2022

View full text Add to dashboard Cite

show abstract

“…In this regard, different nanoparticles (NPs) have been successfully synthesized to load TDF. Chitosan-based nanoparticles coupled with TDF was prepared, characterized and used for optimal oral absorption in experimental rats 27 . Also, Pokharkar and Co-workers fabricated polymer-lipid nanocarrier to deliver TDF intranasally 28 .…”

Section: Introductionmentioning

confidence: 99%

Testicular ultrastructure and hormonal changes following administration of tenofovir disoproxil fumarate-loaded silver nanoparticle in type-2 diabetic rats

Olojede

Lawal

Faborode

et al. 2022

Sci Rep

View full text Add to dashboard Cite

Reproductive dysfunctions (RDs) characterized by impairment in testicular parameters, and metabolic disorders such as insulin resistance and type 2 diabetes mellitus (T2DM) are on the rise among human immunodeficiency virus (HIV) patients under tenofovir disoproxil fumarate (TDF) and highly active antiretroviral therapy (HAART). These adverse effects require a nanoparticle delivery system to circumvent biological barriers and ensure adequate ARVDs to viral reservoir sites like testis. This study aimed to investigate the effect of TDF-loaded silver nanoparticles (AgNPs), TDF-AgNPs on sperm quality, hormonal profile, insulin-like growth factor 1 (IGF-1), and testicular ultrastructure in diabetic rats, a result of which could cater for the neglected reproductive and metabolic dysfunctions in HIV therapeutic modality. Thirty-six adult Sprague–Dawley rats were assigned to diabetic and non-diabetic (n = 18). T2DM was induced by fructose-streptozotocin (Frt-STZ) rat model. Subsequently, the rats in both groups were subdivided into three groups each (n = 6) and administered distilled water, TDF, and TDF-AgNP. In this study, administration of TDF-AgNP to diabetic rats significantly reduced (p < 0.05) blood glucose level (268.7 ± 10.8 mg/dL) from 429 ± 16.9 mg/dL in diabetic control and prevented a drastic reduction in sperm count and viability. More so, TDF-AgNP significantly increased (p < 0.05) Gonadotropin-Releasing Hormone (1114.3 ± 112.6 µg), Follicle Stimulating Hormone (13.2 ± 1.5 IU/L), Luteinizing Hormone (140.7 ± 15.2 IU/L), testosterone (0.2 ± 0.02 ng/L), and IGF-1 (1564.0 ± 81.6 ng/mL) compared to their respective diabetic controls (383.4 ± 63.3, 6.1 ± 1.2, 76.1 ± 9.1, 0.1 ± 0.01, 769.4 ± 83.7). Also, TDF-AgNP treated diabetic rats presented an improved testicular architecture marked with the thickened basement membrane, degenerated Sertoli cells, spermatogenic cells, and axoneme. This study has demonstrated that administration of TDF-AgNPs restored the function of hypothalamic-pituitary–gonadal axis, normalized the hormonal profile, enhanced testicular function and structure to alleviate reproductive dysfunctions in diabetic rats. This is the first study to conjugate TDF with AgNPs and examined its effects on reproductive indices, local gonadal factor and testicular ultrastructure in male diabetic rats with the potential to cater for neglected reproductive dysfunction in HIV therapeutic modality.

show abstract

“…The optimized freeze dried ECONPs were kept in sealed glass vials (n=3) and were stored at 25±2°C with a relative humidity (RH) of 60±5% for 3 months in stability chamber (Remi, Mumbai, India). Samples were collected at a monthly interval and evaluated for morphology, zeta potential, FTIR, drug content, and DR [29].…”

Section: Stability Studiesmentioning

confidence: 99%

Process of Orlistat-Loaded Chitosan Nanoparticles Using Box–behnken Design – An Evaluation Study

Yelavarthi

Devanna

2021

Asian J Pharm Clin Res

View full text Add to dashboard Cite

Objective: High lipophilicity and extensive hepatic metabolism limit oral application of orlistat in obesity treatment. Orlistat-loaded chitosan nanoparticles (CONPs) were optimized by 3-factor 3-level Box–Behnken design (BBD) and surfaced engineered to address limitations. Methods: CONPs were prepared by ionic gelation method. Amounts of chitosan (X1), sodium tripoly phosphate (X2), and orlistat (X3) were selected as independent factors, whereas % entrapment efficiency (Y1) and % drug release (Y2) were employed as responses in BBD. Three-dimensional response surface plots were run to understand the main interaction and quadratic effects of independent variables. Further optimized formulation was surface engineered by Eudragit L-100 (ECONPs) and characterized by FTIR, DSC, XRD, particle size, zeta potential, and SEM. Entrapment efficiency, release kinetics, stability, and in vitro cell line studies were carried out. Results: ECONPs were produced with an average size of 534.6 nm, zeta potential of +5.7 mV, EE of 78.62%, and DR of 80.86%. Eudragit coated CONPs anchored the release of orlistat at pH 6.8 desirable for duodenal targeting. Orlistat was released with low, burst, and sustained release manner over 24 h period followed first-order kinetics with Higuchi model with drug content of 84.87% and 78.44% of release. ECONPs possessed lipase inhibition with IC50 value of 8.0 μg/ml and viability against selected cell lines with CTC50 values (26.32–32.21 μg/ml). Conclusion: BBD was a promising tool in elucidating the insights of formulation variables of CONPs. ECONPs fulfilled the rationale of orlistat release, lipase inhibition, and viability against selected cell lines.

show abstract

Chitosan nanoparticles for the oral delivery of tenofovir disoproxil fumarate: formulation optimization, characterization and ex vivo and in vivo evaluation for uptake mechanism in rats

Abstract: These results show the ability of the designed chitosan based nanoparticles in enhancing the oral absorption of TDF along the oral route by utilizing the active endocytic uptake pathways.

Cited by 28 publications

References 45 publications

Fabrication of PEGylated Chitosan Nanoparticles Containing Tenofovir Alafenamide: Synthesis and Characterization

Fabrication of PEGylated Chitosan Nanoparticles Containing Tenofovir Alafenamide: Synthesis and Characterization

Testicular ultrastructure and hormonal changes following administration of tenofovir disoproxil fumarate-loaded silver nanoparticle in type-2 diabetic rats

Process of Orlistat-Loaded Chitosan Nanoparticles Using Box–behnken Design – An Evaluation Study

Contact Info

Product

Resources

About