Enhanced oral bioavailability of nevirapine within micellar nanocarriers compared with Viramune ®

Morettón, Marcela A.; Cohen, Laura; Lepera, L.G.; Bernabeu, Ezequiel; Taira, Carlos A.; Höcht, Christián; Chiappetta, Diego Andrés

doi:10.1016/j.colsurfb.2014.06.046

Cited by 27 publications

(9 citation statements)

References 41 publications

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“…For the nanomicelle assembly, a low critical micelle concentration (CMC) is critical to the stability during the blood circulation after drug administration [24][25][26]. The present study indicates that the functional docetaxel nanomicelles are stable during drug administration because the nanomicelle material soluplus has a low-CMC value of 7.6 mgÁL À1 [27,28].…”

Section: Discussionmentioning

confidence: 88%

Development of functional docetaxel nanomicelles for treatment of brain glioma

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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The efficacy of anticancer drugs is rather limited in the treatment of brain glioma due to the hindrance of the blood-brain barrier (BBB). Herein, we reported an easy formulation of functional docetaxel nanomicelles for the treatment of brain glioma using a graft copolymer soluplus as basic material through dual-modifications with a glucose-lipid derivative and a dequalinium-lipid derivative. The studies were performed on brain glioma U87MG cells, in vitro BBB models and brain glioma-bearing nude mice. The functional docetaxel nanomicelles were approximately 100 nm. The results demonstrated that the functional docetaxel nanomicelles could transport across the BBB, enhance the cellular uptake, target to the mitochondria, induce the apoptosis, increase the cytotoxicity in the brain glioma cells, and extend survival span of the brain glioma-bearing mice. The action mechanisms were associated with dual-modifications by the glucose-lipid derivative and the dequalinium-lipid derivative, both of which are beneficial for the transport across the BBB. Furthermore, the modification with dequalinium-lipid derivative was able to target to the brain glioma cells and to the mitochondria. In conclusion, the functional docetaxel nanomicelles would be a promising formulation for the treatment of brain glioma, deserving further development for clinical trials.

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Section: Discussionmentioning

confidence: 88%

Development of functional docetaxel nanomicelles for treatment of brain glioma

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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“…Hence, the addition of hydrophilic additives as polymers could interact with the micellar corona, according with their water affinity, and this interaction would influence the final Dh values. An example of this kind of interaction is the addition of glycols and PEG 400 to poloxamers and poloxamines [ 46 ].…”

Section: Resultsmentioning

confidence: 99%

Inhalable Mannosylated Rifampicin–Curcumin Co-Loaded Nanomicelles with Enhanced In Vitro Antimicrobial Efficacy for an Optimized Pulmonary Tuberculosis Therapy

et al. 2022

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Among respiratory infections, tuberculosis was the second deadliest infectious disease in 2020 behind COVID-19. Inhalable nanocarriers offer the possibility of actively targeting anti-tuberculosis drugs to the lungs, especially to alveolar macrophages (cellular reservoirs of the Mycobacterium tuberculosis). Our strategy was based on the development of a mannose-decorated micellar nanoformulation based in Soluplus® to co-encapsulate rifampicin and curcumin. The former is one of the most effective anti-tuberculosis first-line drugs, while curcumin has demonstrated potential anti-mycobacterial properties. Mannose-coated rifampicin (10 mg/mL)–curcumin (5 mg/mL)-loaded polymeric micelles (10% w/v) demonstrated excellent colloidal properties with micellar size ~108 ± 1 nm after freeze-drying, and they remain stable under dilution in simulated interstitial lung fluid. Drug-loaded polymeric micelles were suitable for drug delivery to the deep lung with lung accumulation, according to the in vitro nebulization studies and the in vivo biodistribution assays of radiolabeled (99mTc) polymeric micelles, respectively. Hence, the nanoformulation did not exhibit hemolytic potential. Interestingly, the addition of mannose significantly improved (5.2-fold) the microbicidal efficacy against Mycobacterium tuberculosis H37Rv of the drug-co-loaded systems in comparison with their counterpart mannose-free polymeric micelles. Thus, this novel inhaled nanoformulation has demonstrated its potential for active drug delivery in pulmonary tuberculosis therapy.

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“…Suspensions of solid NV-SDLF and the pure drug were prepared in 0.5% carboxymethyl cellulose with gentle agitation. A test group of animals was administered with solid NV-SDLF suspension and a control group of animals was administered with the pure drug at a dose of 60 mg/ kg body weight with oral gavage (Inugala et al, 2015;Moretton et al, 2014;Usach and Peris, 2011).…”

Section: In-vivo Pharmacokinetic Studies In the Animal Modelmentioning

confidence: 99%

“…In addition to the mentioned toxicity, nevirapine belongs to the Biopharmaceutics Classification System (BCS) class II drugs for the reasons of poor water solubility (~0.1 mg/ml)and pH-dependent solubility with a pKa of 2.8 (Chadha et al, 2010;Moretton et al, 2014). In an acid medium, the solubility is 4.99 g/l and the solubility is reduced by a factor of 10-40 when pH is increased.…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of novel self-dispersing lipid formulation of nevirapine for oral delivery

Bellaiah¹,

Shivakumar²,

Ravi³

2022

J Appl Pharm Sci

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Nevirapine, a non-nucleoside reverse transcriptase inhibitor, exhibits pH-dependent solubility resulting in poor dissolution limiting its absorption. In the present study, an attempt is made to prepare a self-dispersing lipid formulation (SDLF) involving the novel combination of two drug solubility enhancing strategies, i.e., self-emulsifying system (SES) and solid dispersion (SD). Nevirapine-SES (NV-SES) consisting of an ideal ratio of oleic acid (oil), Cremophor RH 40 (surfactant), and Transcutol (co-surfactant) exhibited good emulsifying properties with maximum drug loading. The NV-SES developed was mixed with an equal quantity of nevirapine: gelucire 50/13 solid dispersion [Nevirapine Solid Dispersion (NV-SD)] to get a novel nevirapine SDLF (NV-SDLF). The NV-SDLF was characterized for its zeta potential, polydispersity index, and particle size, and the results obtained were found to be satisfactory. NV-SDLF was adsorbed on carrier neuciline U2 to get solid NV-SDLF, and solid-state characterization using Differential Scanning Calorimetry (DSC) and Powder X-Ray Diffraction (PXRD) indicated the amorphous nature of the drug in NV-SDLF. The in-vitro drug release of the NV-SDLF was found to be 87.2% ± 0.96% in comparison with nevirapine 28.8% ± 1.02%. In-vivo pharmacokinetic performance of solid NV-SDLF and pure drug suspension was carried out in rats, and a significant two-fold increase (p < 0.05) in area under the curve (AUC) of solid NV-SDLF was observed with respect to nevirapine AUC. Thus, the in-vitro and in-vivo results confirmed that the combined strategies of SES and SD in the formulation of solid NV-SDLF were found to enhance the bioavailability of nevirapine, which could be a promising novel drug delivery system in the management of Acquired Immune Deficiency Syndrome (AIDS).

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Enhanced oral bioavailability of nevirapine within micellar nanocarriers compared with Viramune ®

Cited by 27 publications

References 41 publications

Development of functional docetaxel nanomicelles for treatment of brain glioma

Development of functional docetaxel nanomicelles for treatment of brain glioma

Inhalable Mannosylated Rifampicin–Curcumin Co-Loaded Nanomicelles with Enhanced In Vitro Antimicrobial Efficacy for an Optimized Pulmonary Tuberculosis Therapy

Preparation and evaluation of novel self-dispersing lipid formulation of nevirapine for oral delivery

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