Nanoparticle-based vaginal drug delivery systems for HIV prevention

Mallipeddi, Rama; Rohan, Lisa C.

doi:10.1517/17425240903338055

Cited by 77 publications

(72 citation statements)

References 90 publications

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“…29,30 However, the drug release kinetics as well as drug loading could be improved by increasing the size of the nanoparticles. 31 It was found in our preliminary study that spray-dried NCs exhibited an average size ranging between 100 and 500 nm; therefore, our optimization goal was set to maximize EE% while minimize size within this range as further specified in the Results and Discussion section.…”

Section: Box-behnken Experimental Designmentioning

confidence: 99%

Optimization of Formulation Variables Affecting Spray-Dried Oily Core Nanocapsules by Response Surface Methodology

Zhang¹,

Murowchick

Youan³

2011

Journal of Pharmaceutical Sciences

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Section: Box-behnken Experimental Designmentioning

confidence: 99%

Optimization of Formulation Variables Affecting Spray-Dried Oily Core Nanocapsules by Response Surface Methodology

Zhang¹,

Murowchick

Youan³

2011

Journal of Pharmaceutical Sciences

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“…In recent years, studies have reported that the small size of nanocapsules enables them to penetrate cells and deliver drugs intracellularly without suffering extracellular degradation. 43,44 Moreover, controlled release systems can prolong the release and increase the contact time between the drug and the skin. 21 In addition, LNC-Hst increased the retention of the drug in the stratum corneum, possibly due to its rigid structure, 45 which maintains controlled release of the drug in the skin.…”

mentioning

confidence: 99%

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Menezes

Frank

Lima

et al. 2017

IJN

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Chronic venous insufficiency is characterized by chronic reflux disorder of blood from the peripheral to the central vein, with subsequent venous hypertension and resulting changes in the skin. Traditionally, nonsurgical treatments relied on the use of compression therapy, and more recently a variety of flavonoids have been shown to have positive effects. There have also been developments of more effective drug delivery systems using various textiles and nanotechnology to provide new therapeutic options. Our objective was to use nanotechnology to develop a new formulation containing hesperetin (Hst), a substance not previously used in the treatment of chronic venous insufficiency, impregnated into textile fibers as a possible alternative treatment of venous diseases. We prepared the nanocapsules using the interfacial deposition of preformed polymer method with an Hst concentration of 0.5 mg/mL and then characterized the size and distribution of particles. To quantify the Hst in the samples, we developed an analytical method using high-performance liquid chromatography. Studies of encapsulation efficiency (98.81%±0.28%), microscopy, drug release (free-Hst: 104.96%±12.83%; lipid-core nanocapsule-Hst: 69.90%±1.33%), penetration/permeation, drug content (0.46±0.01 mg/mL) and the effect of washing the textile after drug impregnation were performed as part of the study. The results showed that nanoparticles of a suitable size and distribution with controlled release of the drug and penetration/permeation into the skin layers were achieved. Furthermore, it was established that polyamide was able to hold more of the drug, with a 2.54 times higher content than the cotton fiber; after one wash and after five washes, this relation was 2.80 times higher. In conclusion, this is a promising therapeutic alternative to be further studied in clinical trials.

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“…39 Previous studies have established effective and safe intracellular delivery of antiretroviral drugs into human peripheral blood mononuclear cells or human monocyte/macrophage by NPs. 40,41 Further studies have also demonstrated favorable antiretroviral efficacy against HIV-1 when the drug is delivered into human monocyte-derived macrophages.…”

Section: Discussionmentioning

confidence: 99%

Novel intravaginal nanomedicine for the targeted delivery of saquinavir to CD4+ immune cells

Yang¹,

Chen²,

Gu³

et al. 2013

IJN

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Abstract:The goal of this study was to develop and characterize an intravaginal nanomedicine for the active targeted delivery of saquinavir (SQV) to CD4+ immune cells as a potential strategy to prevent or reduce HIV infection. The nanomedicine was formulated into a vaginal gel to provide ease in self-administration and to enhance retention within the vaginal tract. SQV-encapsulated nanoparticles (SQV-NPs) were prepared from poly(lactic-co-glycolic acid) (PLGA) and conjugated to antihuman anti-CD4 antibody. Antibody-conjugated SQV-NPs (Ab-SQV-NPs) had an encapsulation efficiency (EE%) of 74.4% ± 3.7% and an antibody conjugation efficiency (ACE%) of 80.95% ± 1.10%. Over 50% of total loaded SQV was released from NPs over 3 days. NPs were rapidly taken up by Sup-T1 cells, with more than a twofold increase in the intracellular levels of SQV when delivered by Ab-SQV-NPs in comparison to controls 1 hour post-treatment. No cytotoxicity was observed when vaginal epithelial cells were treated for 24 hours with drug-free Ab-NPs (1,000 µg/mL), 1% HEC placebo gel (200 mg/mL), or 1% HEC gel loaded with drug-free Ab-NPs (5 mg NPs/g gel, 200 mg/mL of gel mixture). Overall, we described an intravaginal nanomedicine that is nontoxic and can specifically deliver SQV into CD4 + immune cells. This platform may demonstrate potential utility in its application as postexposure prophylaxis for the treatment or reduction of HIV infection, but further studies are required.

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Nanoparticle-based vaginal drug delivery systems for HIV prevention

Abstract: To date, few studies have been published that exploit nanoparticle-based microbicidal delivery to the vagina. The use of nanoparticles for vaginal drug delivery provides an approach to overcome the existing barriers to success.

Cited by 77 publications

References 90 publications

Optimization of Formulation Variables Affecting Spray-Dried Oily Core Nanocapsules by Response Surface Methodology

Optimization of Formulation Variables Affecting Spray-Dried Oily Core Nanocapsules by Response Surface Methodology

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Novel intravaginal nanomedicine for the targeted delivery of saquinavir to CD4+ immune cells

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