Tenofovir disoproxil fumarate loaded PLGA nanoparticles for enhanced oral absorption: Effect of experimental variables and in vitro, ex vivo and in vivo evaluation

Shailender, Joseph; Ravi, Punna Rao; Saha, Paramita; Dalvi, Avantika; Myneni, Srividya

doi:10.1016/j.colsurfb.2017.07.037

Cited by 22 publications

(17 citation statements)

References 40 publications

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“…Compared to the epirubicin solution, a 4.49-fold higher permeation of epirubicin across the rat ileum was achieved by this nanoformulation, which also contributed to a 3.9-fold improvement of relative oral bioavailability. In addition, the PLGA nanoformulation was applied to improve the oral absorption of tenofovir disoproxil fumarate [48]. The everted gut sac study proved that using PLGA nanoparticles as a carrier significantly increased the transport flux by fivefold, and the in vivo pharmacokinetic study also demonstrated this formulation efficiently improve the relative oral bioavailability by 6.79-fold when compared with the unformulated drug.…”

Section: Storage and Ph Stabilities Of Fst-npmentioning

confidence: 99%

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

et al. 2021

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This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of −29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.

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Section: Storage and Ph Stabilities Of Fst-npmentioning

confidence: 99%

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

et al. 2021

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“…The spectra of pure drug showed a sharp endothermic peak at 118.1 °C corresponding to its melting point temperature which is around 115 °C. But this endothermic peak was found to be absent in the spectra of TDF ACNs with either of the polymers, which indicated that the drug was in no more crystalline state in the ACNs, instead it might be in either molecular dispersion or amorphous form (Shailender et al, 2017). This might be attributed to the mode of incorporation of drug i.e.…”

Section: Experimental Designmentioning

confidence: 94%

Study on influence of polymer and surfactant on in vitro performance of biodegradable aqueous-core nanocapsules of tenofovirdisoproxil fumarate by response surface methodology

Srikar

Rani

2019

Braz. J. Pharm. Sci.

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The major objective of this study was to investigate the effect of biodegradable polymer type and surfactant concentration on various characteristics viz. particle size, entrapment efficiency and drug release rate constant of aqueous core nanocapsules (ACNs) containing tenofovirdisoproxil fumarate. In this study, the nanocapsules were prepared by modified multiple emulsion technique with biodegradable polymers viz. poly(lactide-co-glycolide) of two different grades (PLGA RG502H and PLGA RG503H) and poly lactic acid (PLA R203H); and the surfactant employed was span 80. The experiments were designed under response surface methodology by employing the Design Expert software. Entrapment efficiency, particle size and drug release rate constant were taken as response variables. The prepared nanocapsules were subjected to characterization studies and the obtained results were statistically analyzed by Analysis of Variance (ANOVA) for response surface 2-Factorial Interaction model. ANOVA studies showed that the influence of both factors on all the response variables were significant at p<0.05. The optimized formulation was found to have the entrapment efficiency of 71.58%, particle size of 252.41 nm and the drug release rate constant of 0.045 h-1 ; thus, indicating that the ACNs were obtained with finest characteristics. SEM studies showed that the particles were spherical.

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“…A similar approach was exploited for the incorporation of TAF and elvitegravir, an integrase inhibitor, during the fabrication of devices to be used during vaginal prevention [123,124]. The drug absorption following oral administration were also positively affected by the use of TAF/PGLA loaded NPs, as highlighted by a statistical model study [125]. Formulations containing mono- or by-layered films of PVA and pectin were coupled with Eudragit NPs loaded with TDF/FTC, by nano spray-drying technique.…”

Section: Nucleoside Reverse Transcriptase Inhibitors Nanosystemsmentioning

confidence: 99%

Reverse Transcriptase Inhibitors Nanosystems Designed for Drug Stability and Controlled Delivery

et al. 2019

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An in-depth analysis of nanotechnology applications for the improvement of solubility, distribution, bioavailability and stability of reverse transcriptase inhibitors is reported. Current clinically used nucleoside and non-nucleoside agents, included in combination therapies, were examined in the present survey, as drugs belonging to these classes are the major component of highly active antiretroviral treatments. The inclusion of such agents into supramolecular vesicular systems, such as liposomes, niosomes and lipid solid NPs, overcomes several drawbacks related to the action of these drugs, including drug instability and unfavorable pharmacokinetics. Overall results reported in the literature show that the performances of these drugs could be significantly improved by inclusion into nanosystems.

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Tenofovir disoproxil fumarate loaded PLGA nanoparticles for enhanced oral absorption: Effect of experimental variables and in vitro, ex vivo and in vivo evaluation

Cited by 22 publications

References 40 publications

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

Study on influence of polymer and surfactant on in vitro performance of biodegradable aqueous-core nanocapsules of tenofovirdisoproxil fumarate by response surface methodology

Reverse Transcriptase Inhibitors Nanosystems Designed for Drug Stability and Controlled Delivery

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