Intranasal Administration of Antiretroviral-Loaded Micelles for Anatomical Targeting to The Brain in HIV

Chiappetta, Diego Andrés; Höcht, Christián; Opezzo, Javier A.W.; Sosnik, Alejandro

doi:10.2217/nnm.12.104

Cited by 89 publications

(51 citation statements)

References 74 publications

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“…In vitro study: male 3-month-old Wistar rats [68] Saquinavir Combination of PEI/γ-PGA/PLGA NPs increased the permeability of drug across the blood-brain barrier in vitro…”

Section: Efv Intranasal Administration Of Efv Loaded Micelles For Tarmentioning

confidence: 99%

Nanodrug Formulations to Enhance HIV Drug Exposure in Lymphoid Tissues and Cells: Clinical Significance and Potential Impact on Treatment and Eradication of HIV/AIDS

Shao

Kraft

et al. 2016

Nanomedicine (Lond.)

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Although oral combination antiretroviral therapy effectively clears plasma HIV, patients on oral drugs exhibit much lower drug concentrations in lymph nodes than blood. This drug insufficiency is linked to residual HIV in cells of lymph nodes. While nanoformulations improve drug solubility, safety and delivery, most HIV nanoformulations are intended to extend plasma levels. A stable nanodrug combination that transports, delivers and accumulates in lymph nodes is needed to clear HIV in lymphoid tissues. This review discusses limitations of current oral combination antiretroviral therapy and advances in anti-HIV nanoformulations. A ‘systems approach’ has been proposed to overcome these limitations. This concept has been used to develop nanoformulations for overcoming drug insufficiency, extending cell and tissue exposure and clearing virus for treating HIV/AIDS.

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“…In vitro study: male 3-month-old Wistar rats [68] Saquinavir Combination of PEI/γ-PGA/PLGA NPs increased the permeability of drug across the blood-brain barrier in vitro…”

Section: Efv Intranasal Administration Of Efv Loaded Micelles For Tarmentioning

confidence: 99%

Nanodrug Formulations to Enhance HIV Drug Exposure in Lymphoid Tissues and Cells: Clinical Significance and Potential Impact on Treatment and Eradication of HIV/AIDS

Shao

Kraft

et al. 2016

Nanomedicine (Lond.)

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“…To overcome these problems present research aims at incorporating 6-SRGO within polymers to develop a drug delivery system displaying enhanced drug solubility, while reducing systemic toxicity of 6-SRGO. Mixed micelles; a system for the solubilisation of water-insoluble drugs to increase its efficacy [20,21] is known for its stability and its ability to solubilize maximum amount of water-insoluble drugs in their inner core [22]. Mixed micelles are smaller in size and having outer hydrophilic shell which is responsible for prolonged circulation times in vivo and results in accumulation in the tumoral tissues.…”

Section: Introductionmentioning

confidence: 99%

6-Shogaol Rich Ginger Oleoresin Loaded Mixed Micelles Enhances in Vitro Cytotoxicity on McF-7 Cells and in Vivo Anticancer Activity Against Dal Cells

Kemkar

Lohidasan

Sathiyanarayanan

et al. 2018

Int J Pharm Pharm Sci

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Objective: Ginger oleoresin (GO) plays an important role on the attenuation of complications associated to the cancer which is attributed to 6-shogaol (6-SGL). The major challenge in using 6-SGL for therapeutic applications is its poor aqueous solubility, low stability in GI and low bioavailability. Considering the potent anticancer nature of 6-SGL and its synergistic activity with other constituents in GO, there is a need to develop a suitable drug delivery system. Methods:Thus in the present study, 6-SGL rich GO (6-SRGO) was incorporated into mixed micelles using phospholipid (Soya Lecithin) as a carrier. The prepared 6-SRGO loaded mixed micelles (6-SRGO-LMM) were characterized physically and chemically using Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and further evaluated for stability study, in vitro release study, in vitro cytotoxicity study and in vivo anticancer activity in comparison with 6-SRGO. Results:The composition such as, drug content (86.27±1.56), encapsulation efficiency (81.55±1.05) and particle size (356.11±4.07) were optimized using 3 2 Conclusion:We have developed and investigated mixed micelles composed of phospholipids (soya lecithin S80) and SCH as an effective nanocarrier for the delivery of a natural lipophilic anticancer bioactive 6-SGL from 6-SRGO. factorial design. FTIR and DSC study confirm that the 6-SGL from 6-SRGO was entrapped in the core of phospholipid by self-assembly method to form mixed micelles. The 6-SRGO-LMM exhibited significant in vitro (GI50-23.2 μg/ml) and in vivo anticancer activity in comparison with 6-SRGO.

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“…According to Hanson and Frey, IN delivery of ARV could be used in prevention and treatment of neuro-AIDS [5]. Literature indicates successful delivery ARV by IN routes, Abeer M. Al-Ghananeem and coworkers [6] have formulated didanosine-chitosan nanoparticles with increased drug delivery in the CNS, Barbi et al [7] prepared zidovudinchitosan nanoparticles for IN delivery, Dalpiaz A. and coworkers has conjugated zidovudine to ursodeoxycholic acid to produce prodrug which remained in murine macrophages 20 times higher than zidovudine and designed chitosan chloride microparticles had more CSF uptake in rat [8], Mahajan et al [9] developed saquinavir mesylate nanoemulsion and Chiappetta et al [10] developed efavirenz poly(ethylene oxide)-poly(propylene oxide) polymeric micelles with fivefold increase in bioavailability of drug compared to intravenous (i.v.) administration.…”

Section: Introductionmentioning

confidence: 99%

Intranasal chitosan-g-HPβCD nanoparticles of efavirenz for the CNS targeting

Belgamwar¹,

Khan²,

Yeole

2017

Artificial Cells, Nanomedicine, and Biotechnology

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Incompetence of antiretrovirals (ARV) in complete eradication of HIV from the CNS is the biggest issue in neuro-AIDS treatment. The ineffectiveness is largely due to the poor penetration of ARV. Hence, the present study is attempted to enhance the CNS uptake of efavirenz (EFV) by designing intranasal EFV nanoparticles (EFV-NPs). EFV-NPs were fabricated using chitosan-g-HPβCD by ionic gelation method and optimized using quadratic response surface methodology (RSM) employing two-factor, five-level circumscribed central composite design. NPs containing drug: polymer ratio (1.25:0.79) were spherical with 198 ± 4.4 nm size, 23.28 ± 1.5% drug loading and 38 ± 1.43% entrapment efficiency. NPs showed sustained drug release (99.03 ± 0.30% in 8 h) and followed Fickian diffusion mechanism. It gave 4.76 times greater permeability than plain drug solution through porcine nasal mucosa. Enhanced CNS bioavailability (12.40-fold that of i.v solution) of EFV, high drug-targeting percentage (99.24%) and drug-targeting index (141.3) post-intranasal administration of NPs was observed. These results are corroborated by gamma scintigraphy images, which revealed high CNS uptake. NPs appeared histocompatible with porcine nasal mucosa and non-toxic to L929 cell line. Thus, CS-g-HPβCD served as a potential carrier in developing intranasal mucoadhesive EFV-NPs for the CNS targeting.

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Intranasal Administration of Antiretroviral-Loaded Micelles for Anatomical Targeting to The Brain in HIV

Abstract: These findings demonstrate the potential of this scalable and cost-viable strategy to address the HIV sanctuary in the CNS.

Cited by 89 publications

References 74 publications

Nanodrug Formulations to Enhance HIV Drug Exposure in Lymphoid Tissues and Cells: Clinical Significance and Potential Impact on Treatment and Eradication of HIV/AIDS

Nanodrug Formulations to Enhance HIV Drug Exposure in Lymphoid Tissues and Cells: Clinical Significance and Potential Impact on Treatment and Eradication of HIV/AIDS

6-Shogaol Rich Ginger Oleoresin Loaded Mixed Micelles Enhances in Vitro Cytotoxicity on McF-7 Cells and in Vivo Anticancer Activity Against Dal Cells

Intranasal chitosan-g-HPβCD nanoparticles of efavirenz for the CNS targeting

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