Polymeric Nanoparticles for Enhancing Antiretroviral Drug Therapy

Govender, Thirumala; Ojewole, Elizabeth; Naidoo, Pragalathan; Mackraj, Irene

doi:10.1080/10717540802321776

Cited by 47 publications

(19 citation statements)

References 48 publications

(51 reference statements)

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“…Various nanotechnology-based systems are studied extensively by scientists to address the specific issues associated with antiretroviral therapy (Govender et al, 2008). Polymeric NPs-containing antiretroviral drugs can overcome the drawback of physiological stability as well as drug loading.…”

Section: Introductionmentioning

confidence: 99%

Bioavailability enhancement, Caco-2 cells uptake and intestinal transport of orally administered lopinavir-loaded PLGA nanoparticles

2016

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Nanoparticles (NPs) can be absorbed via M cells of Peyer's patches after oral delivery leading to passive lymphatic targeting followed by systemic drug delivery. Hence, the study was aimed to formulate PLGA NPs of lopinavir. The NPs were prepared by nanoprecipitation, optimized by 3 3 factorial design and characterized by TEM, DSC, FTIR studies and safety was assessed by MTT assay. In vivo pharmacokinetic studies were performed in rats. The NPs were discrete spherical structures having particle size of 142.1 ± 2.13 nm and entrapment of 93.03 ± 1.27%. There was absence of drug-polymer interaction. Confocal images revealed the penetration and absorption of coumarin-loaded NPs in Caco-2 cells and intestine after oral delivery. There was 3.04 folds permeability and 13.9 folds bioavailability enhancement from NPs. The NPs can be promising delivery system for antiretroviral drug by delivering the drug to lymph (major HIV reservoir site) via direct absorption through intestine before reaching systemic circulation.

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Section: Introductionmentioning

confidence: 99%

Bioavailability enhancement, Caco-2 cells uptake and intestinal transport of orally administered lopinavir-loaded PLGA nanoparticles

2016

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“…Polymethacrylates are widely used in pharmaceutical delivery systems for sustained drug delivery, 10) hot melt extrusion, 11,12) microencapsulation, 13) nanoparticle, 14,15) antiretroviral drug delivery, 15,16) floating microspheres, 17) colon delivery 18,19) and transdermal drug delivery. 20) In our previous studies we showed the effect of thermal treating on the release of indomethacin 8) and diclofenac sodium 9) from acrylic matrix tablets and mechanistically studied the effect of heat-treating on physicochemical structure of tablet.…”

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confidence: 99%

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Hasanzadeh

Ghaffari

Monajjemzadeh

et al. 2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of the present study was to investigate the effect of thermal-treating on the release of ibuprofen from the granules prepared using aqueous dispersions of Eudragit. To accomplish this goal, different formulations were prepared using wet granulation method containing two different types of Eudragit aqueous dispersions, RS30D, RL30D and Avicel as filler. Tablets were prepared using direct compression method. The prepared tablets were thermally treated at 50 and 70°C for 24 h. The drug release from tablets was assessed before and after thermal-treating. The results of release study showed that, thermally-treating the tablets at the temperatures higher than glass transition temperature (Tg) of the polymer can decrease the drug release from matrices. For mechanistic evaluation of the effect of thermal-treating, powder X-ray diffraction (XPD), scanning electron microscopy (SEM), differential scanning calorimeter (DSC), Fourier transform infrared (FT-IR) and helium pycnometer have been employed. The SEM graphs showed that the tablets have smoother surface with less porosity after thermal-treating. FT-IR spectra showed no change in the spectrum of thermally-treated tablet compared to control. In DSC graphs, no crystalline change was seen in the heat-treated samples of ibuprofen tablets, but decreased and widened peak size were related to the probable formation of solid solution of ibuprofen in Eudragit matrix. The results of helium pycnometer showed a significant decrease in the total porosity of some heat-treated samples. This study revealed the importance of thermal treating on the drug release from sustained release tablets containing Eudragit polymer.

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“…In order to overcome these problems, several new chemical entities or improved delivery systems have been proposed involving the use of several nanotechnology-based delivery systems [10][11][12][13][14]. Thus, in order to improve HIV therapy, a large number of carriers have been developed; they include polymeric nanoparticles, solid lipid nanoparticles, liposomes, nanoemulsions, dendrimers, and drug conjugates [15][16][17][18][19][20]. These nanotechnology carriers are able to deliver the HIV current drugs in a controlled and/or targeted manner thereby increasing the drug bioavailability and residence time at target sites with a considerable improvement in life quality of HIV patients.…”

Section: Introductionmentioning

confidence: 99%

Nanotechnology Approaches for Antiretroviral Drugs Delivery

Iannazzo¹,

Pistone²,

Romeo³

et al. 2015

Journal of AIDS and HIV infections

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The development of effective drug delivery approaches for the treatment of AIDS and HIV infection is a global challenge. The advent of multidrug, highly active antiretroviral therapy (HAART), have increased the life span of HIV-infected patients. However, it has not eradicated HIV infections, particularly in anatomically privileged sites, such as the brain, testes, gut, liver, kidney, and secondary lymphoid tissue. Several nanocarriers have been investigated in order to enhance the effective delivery of antiretroviral drugs for HIV prevention and therapy. This review focuses on the most recent and significant examples of nanotechnology-based approaches for the delivery of antiretroviral agents belonging to the classes of nucleoside-analog reverse transcriptase inhibitors (NRTIs) and nonnucleoside reverse transcriptase inhibitors (NNRTIs). Nanocarriers such as natural and synthetic polymeric nanoparticles, dendrimers, liposomes, and various drug conjugates have been discussed. These nanotechnology carriers are able to deliver the antiretroviral agents in a controlled and/or targeted manner thereby increasing the drug bioavailability and residence time at target sites with a considerable improvement in quality of HIV patients.

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Polymeric Nanoparticles for Enhancing Antiretroviral Drug Therapy

Cited by 47 publications

References 48 publications

Bioavailability enhancement, Caco-2 cells uptake and intestinal transport of orally administered lopinavir-loaded PLGA nanoparticles

Bioavailability enhancement, Caco-2 cells uptake and intestinal transport of orally administered lopinavir-loaded PLGA nanoparticles

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Nanotechnology Approaches for Antiretroviral Drugs Delivery

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