Exploring the use of novel drug delivery systems for antiretroviral drugs

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

doi:10.1016/j.ejpb.2008.06.020

Cited by 108 publications

(56 citation statements)

References 99 publications

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“…Following its administration, liposomes are recognized and taken up by cells of the mononuclear phagocytic system. Since the HIV virus localizes in these cells, liposomes therefore represent a suitable drug delivery system for targeting antiretroviral agents into infected cells, and thus have the potential of improving the efficacy of drugs and reducing side effects (9)(10)(11)(12).…”

Section: Introductionmentioning

confidence: 99%

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

Zidan

Spinks

Fortunak

et al. 2010

AAPS J

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Abstract. Near-infrared (NIR) approaches is considered one of the most well-studied process analyzers evolving from the process analytical technology initiatives. The objective of this study was to evaluate NIR spectroscopy and imaging to assess individual components within a novel tenofovir liposomal formulation. By varying stearylamine, as a positive charge imparting agent, five batches were prepared by the thin film method. Each formulation was characterized in terms of drug entrapment efficiency, release characteristics, particle sizing, and zeta potential. Drug excipients compatibility was tested using Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The obtained results showed an increase in drug entrapment and a slower drug release by increasing the incorporated percentage of stearylamine. The compatibility testing revealed a significant interaction between the drug and some of the investigated excipients. The developed NIR calibration model was able to assess drug, phospholipid, and stearylamine levels along the batches. The calibration and prediction plots were linear with correlation coefficients of more than 0.9. The root square standard errors of calibration and prediction did not attain 5% of the measured values confirming the accuracy of the model. In contrast, NIR spectral imaging was capable of clearly distinguishing the different batches, both qualitatively and quantitatively. A linear relationship was obtained correlating the actual drug entrapped and the predicted values obtained from the partial least squares images.

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Section: Introductionmentioning

confidence: 99%

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

Zidan

Spinks

Fortunak

et al. 2010

AAPS J

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show abstract

“…A thorough understanding of the phenomena taking place upon exposure of a given body to a certain pharmacological agent is thus essential for the development of improved controlled release drug formulations. Sustained drug delivery systems are designed to achieve a continuous release of a pharmaceutical agent at a predictable and reproducible kinetics, over an extended period of time, with a consequent minimization of drug-related deleterious side effects and improved patient compliance, which is greater in the case of oral formulations [6][7][8][9] . Since the newly established protocol ruling toxicological tests 10,11 severely limits the use of animals in lethal experiments, there has been an increased interest in in vitro techniques, for obtaining reliable biological data 12,13 .…”

Section: Research Articlementioning

confidence: 99%

New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells

Santos¹,

Pina²,

Marques³

et al. 2012

Drug Development and Industrial Pharmacy

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Objective: The aim of this study was to adjust the zidovudine (AZT) release from solid tablets to an ideal profile, by developing matrices comprising swellable polymers with nonswellable ones.Methods: Directly compressed matrices comprised different ratios of hydroxypropylmethylcellulose K15M and K100M, ethylcellulose, and methacrylic acid (Eudragit® RS PO and Eudragit® RL PO) were prepared. Technological characterization and evaluation of the in vitro release behavior were carried out. Cell density and viability following drug exposure were evaluated by the SRB method, for the Caco-2 line, while cell morphology was assessed upon Trypan blue staining.Results: A specific formulation containing 5% of each excipient − HPMC K15M, HPMC K100M, Eudragit® RS PO, and Eudragit® RL PO − was found to yield the best release profile. Application of the Korsmeyer-Peppas model to the dissolution profile evidenced that a non-Fickian (anomalous) transport is involved in the drug release. Regarding the influence of the tablets' composition on the drug's cytotoxic effect toward the Caco-2 cell line, a reduction of cell biomass (0-15%) was verified for the distinct AZT formulations tested, F19 having displayed the highest cytotoxicity, after 24 and 48 h of incubation. Additionally, a high reversibility of the AZT effect was observed. Conclusions:The results showed that the simultaneous application of both hydrophilic and hydrophobic polymers can modulate the drug release process, leading to an improved efficacy and patient compliance. All AZT formulations studied were found to be cytotoxic against Caco-2 cells, F19 being the most effective one.

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“…Highly active antiretroviral therapy (HAART), which is used to treat human immunodeficiency virus type-1 (HIV-1), has contributed positively to the decline of deaths related to acquired immunodeficiency syndrome (AIDS) [13]. As a result of oral administration and in high concentrations, HAART has been reported to cause unwanted side effects [14]. The literature has suggested drug delivery systems that deposit drugs directly into infected or diseased sites can reduce drug-related toxicities [15].…”

Section: Introductionmentioning

confidence: 99%

Noninvasive micromanipulation of live HIV-1 infected cells via laser light

Mthunzi

2015

AIP Conference Proceedings

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Exploring the use of novel drug delivery systems for antiretroviral drugs

Cited by 108 publications

References 99 publications

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells

Noninvasive micromanipulation of live HIV-1 infected cells via laser light

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