Use Of Nanocarriers Research Articles

Nanomedicine strategies for targeting skin inflammation.

Topical treatment of skin diseases is an attractive strategy as it receives high acceptance from patients, resulting in higher compliance and therapeutic outcomes. Recently, the use of variable nanocarriers for dermal application has been widely explored, as they offer several advantages compared with conventional topical preparations, including higher skin penetration, controlled and targeted drug delivery and the achievement of higher therapeutic effects. This article will focus on skin inflammation or dermatitis as it is one of the most common skin problems, describing the different types and causes of dermatitis, as well as the typical treatment regimens. The potential use of nanocarriers for targeting skin inflammation and the achievement of higher therapeutic effects using nanotechnology will be explored.

Preclinical studies of pegylated- and non-pegylated liposomal forms of doxorubicin as radiosensitizer on orthotopic high-grade glioma xenografts.

Free doxorubicin (DXR) is not currently used to treat brain tumors because (i) the blood-brain barrier limits the drug deposition into the brain (ii) lethal toxic effects occur when combined with radiation therapy. Since encapsulation of DXR within liposomal carriers could overcome these drawbacks, the present study aimed at evaluating the radiosensitizing properties of non-pegylated (NPL-DXR) and pegylated (PL-DXR) liposomal doxorubicin on orthotopic high-grade glioma xenografts (U87). DXR accumulation in brain tissues was assessed by a high-performance liquid chromatography method and antitumor efficacy was evaluated by mice survival determination. We showed that encapsulation of DXR ensured a preferential deposition of DXR in tumoral tissue in comparison with normal brain tissue: the best AUC tumor tissue/AUC normal tissue ratio depended greatly on the schedule. Overall, thanks to the optimization of the delivery schedule, we demonstrated a radiosensitizing effect for both liposomal DXR without toxicity of this combination on the U87 human malignant glioma orthotopic xenografts. This study shows that the use of nanocarriers, allowing targeting of intracerebral tumor, renders relevant the combination of anthracyclin with radiation therapy to treat brain tumors, opening a new field of therapeutic applications. However, our results point out that, for each new delivery system, the administration schedules need to be rigorously optimized.

Nanotechnological Strategies for the Treatment of Neglected Diseases

Neglected diseases are prevalent in less developed countries and are associated with high levels of mortality and/or morbidity. The drugs used in clinical practice are toxic, reducing patient compliance, and generally do not result in a cure, and there has also been a surge in drug resistance. Additionally, a major challenge in drug treatment lies in reaching the intracellular sites infected by parasites. The development of nanotechnology-based drug delivery systems for drugs intended to treat neglected diseases is a promising avenue because the use of nanocarriers presents the ability to target drugs to the infected cells, and the prolonged drug release profile possible with these systems permits longer contact between the drug and the parasite. This review describes the roles of colloidal drug carriers, such as liposomes, polymeric nanoparticles and solid lipid nanoparticles, in research on optimizing the delivery of antileishmanial, antitrypanosomal, antichagasic and antimalarial agents.

Biocompatibility study of two diblock copolymeric nanoparticles for biomedical applications by in vitro toxicity testing

Drugs used for chemotherapy normally carry out adverse, undesired effects. Nanotechnology brings about new horizons to tackle cancer disease with a different strategy. One of the most promising approaches is the use of nanocarriers to transport active drugs. These nanocarriers need to have special properties to avoid immune responses and toxicity, and it is critical to study these effects. Nanocarriers may have different nature, but polypeptide-based copolymers have attracted considerable attention for their biocompatibility, controlled and slow biodegradability as well as low toxicity. Little has been done regarding specific nanocarriers toxicity. In this study, we performed a thorough toxicological study of two different block copolymer nanoparticles (NPs); poly(trimethylene carbonate)-block–poly(l-glutamic acid) (PTMC-b–PGA) and poly(ethylene glycol)-block–poly(γ-benzyl-l-glutamate) (PEG-b–PBLG) with sizes between 113 and 131 nm. Low blood–serum–protein interaction was observed. Moreover, general toxicity assays and other endpoints (apoptosis or necrosis) showed good biocompatibility for both NPs. Reactive oxygen species increased in only two cell lines (HepG2 and TK6) in the presence of PTMC-b–PGA. Cytokine production study showed cytokine induction only in one cell line (A549). We also performed the same assays on human skin organ culture before and after UVB light treatment, with a moderate toxicity after treatment independent of NPs presence or absence. Interleukin 1 induction was also observed due to the combined effect of PEG-b–PBLG and UVB light irradiation. Future in vivo studies for biocompatibility and toxicity will provide more valuable information, but, so far, the findings presented here suggest the possibility of using these two NPs as nanocarriers for nanomedical applications, always taking into account the application procedure and the way in which they are implemented.

Evaluation of chitosan nanoformulations as potent anti-HIV therapeutic systems

BackgroundAntiretroviral Therapy (ART) is currently the major therapeutic intervention in the treatment of AIDS. ART, however, is severely limited due to poor availability, high cytotoxicity, and enhanced metabolism and clearance of the drug molecules by the renal system. The use of nanocarriers encapsulating the anti-retroviral drugs may provide a solution to the aforementioned problems. Importantly, the application of mildly immunogenic polymeric carrier confers the advantage of making the nanoparticles more visible to the immune system leading to their efficient uptake by the phagocytes. MethodsThe saquinavir-loaded chitosan nanoparticles were characterized by transmission electron microscopy and differential scanning calorimetry and analyzed for the encapsulation efficiency, swelling characteristics, particle size properties, and the zeta potential. Furthermore, cellular uptake of the chitosan nanocarriers was evaluated using confocal microscopy and Flow cytometry. The antiviral efficacy was quantified using viral infection of the target cells. ResultsUsing novel chitosan carriers loaded with saquinavir, a protease inhibitor, we demonstrate a drug encapsulation efficiency of 75% and cell targeting efficiency greater than 92%. As compared to the soluble drug control, the saquinavir-loaded chitosan carriers caused superior control of the viral proliferation as measured by using two different viral strains, NL4-3 and Indie-C1, and two different target T-cells, Jurkat and CEM-CCR5. ConclusionChitosan nanoparticles loaded with saquinavir were characterized and they demonstrated superior drug loading potential with greater cell targeting efficiency leading to efficient control of the viral proliferation in target T-cells. General significanceOur data ascertain the potential of chitosan nanocarriers as novel vehicles for HIV-1 therapeutics.

Anti-CD30 antibody conjugated liposomal doxorubicin with significantly improved therapeutic efficacy against anaplastic large cell lymphoma

The use of nano-carriers has been shown to improve the delivery and efficacy of chemotherapeutic agents in cancer patients. Recent studies suggest that decoration of the surface of nano-carriers with various targeting moieties may further improve the overall therapeutic efficacy. In this study, we compared the therapeutic efficacy of Doxil® (commercial doxorubicin-loaded liposomes) and that of Doxil® conjugated with anti-CD30 antibodies (CD30-targeted Doxil®) in treating anaplastic large cell lymphoma (ALCL), a type of T-cell lymphoma characterized by a high CD30 expression. Compared to Doxil®, the CD30-targeted Doxil® showed a significantly higher binding affinity to ALCL cells (5.3% versus 27%, p = 0.005) and a lower inhibitory concentration at 50% (IC50) in-vitro (32.6 μg/mL versus 12.6 μg/mL, p = 0.006). In a SCID mouse xenograft model, CD30-targeted Doxil® inhibited tumor growth more significantly than the unconjugated formulation; specifically, tumors in mice treated with CD30-targeted Doxil® were significantly smaller than those in mice treated with Doxil® (average, 117 mm3 versus 270 mm3, p = 0.001) at 18 days after the tumors were inoculated. Our findings have provided the proof-of-principle of using CD30-targeted nano-carriers to treat cancers that are characterized by a high level of CD30 expression, such as ALCL.

Recent Patents on Common Modifications Made to Traditional Micellar- Based Chemotherapeutics Designed to Improve Drug Delivery

The use of nanocarriers as drug delivery vehicles for chemotherapeutics improves overall pharmacokinetics and biodistribution of otherwise unencapsulated cytotoxic agents, and can significantly decrease unintended negative sideeffects commonly associated with these types of drugs. While a wide variety of nanocarrier-based chemotherapeutics have been reported, micelles are particularly attractive candidates due to inherent characteristics that make them ideal for drug encapsulation. Therefore, it is not surprising that several formulations are currently in various stages of clinical trials. However, while proving to be quite promising, challenges remain involving effective drug transfer from the nanocarrier to cancer cells. Thus, several groups have reported various strategies involving modifications made to these drug delivery vehicles in order to improve delivery of encapsulated cytotoxic agents to tumor cells. While various methods have been reported to achieve this, here we focus specifically on modifications made involving targeting ligand addition, as well as the incorporation of pH-sensitive molecules to these nanocarriers. Recent patents involving these specific modifications made to traditional micelles are discussed in this review. Keywords: Micelles, micellar-based chemotherapeutics, cytotoxic agents, drug carriers, nanocarriers, drug delivery, nanoparticles.

The use of lipid-based nanocarriers for targeted pain therapies

Sustained delivery of analgesic agents at target sites remains a critical issue for effective pain management. The use of nanocarriers has been reported to facilitate effective delivery of these agents to target sites while minimizing systemic toxicity. These include the use of biodegradable liposomal or polymeric carriers. Of these, liposomes present as an attractive delivery system due to their flexible physicochemical properties which allow easy manipulation in order to address different delivery considerations. Their favorable toxicity profiles and ease of large scale production also make their clinical use feasible. In this review, we will discuss the concept of using liposomes as a drug delivery carrier, their in vitro characteristics as well as in vivo behavior. Current advances in the targeted liposomal delivery of analgesic agents and their impacts on the field of pain management will be presented.

Highly bioavailable anticancer herbal-loaded nanocarriers for use against breast and colon cancer in vitro and in vivo systems

This study focused on designing a large-scale producible vehicle for the pharmaceutically important compound berberine, to simultaneously improve its bioavailability against cancer cells and reduce cytotoxicity toward normal cells. This vehicle is composed of chitosan and tripolyphosphate, and was prepared with a simple ionic cross-linking method. The properties of the berberine-loaded chitosan-tripolyphosphate nanoparticles (BB-LCTNP) were dependent on berberine, chitosan, and tripolyphosphate concentrations. The bioavailability improvement and anticancer efficiency of the BB-LCTNPs were analyzed using MDA-MB-435 and Colo-205 cells. The results revealed that the particle size, loading efficiency, and IC50 of the BB-LCTNPs can be controlled easily. The pharmacodynamic availability of berberine increased up to 3 times when loaded into the nanoparticles because they directly targeted cancer cell nuclei. Moreover, the BB-LCTNPs were non-toxic toward normal cells. In vivo studies revealed that BB-LCTNPs can reduce drug dosages up to 3 times and suppress tumor growth. The surfaces of the prepared BB-LCTNPs were modified using mPEG acid, but the in vitro and in vivo studies of these particles are currently ongoing.

Nanocarriers for transdermal drug delivery

Nanocarriers for transdermal drug delivery José Juan Escobar-Chávez,1 Roberto Díaz-Torres,2 Isabel Marlen Rodríguez-Cruz,3 Clara Luisa Domínguez-Delgado,4 Rafael Sampere Morales,5 Enrique Ángeles-Anguiano,6 Luz María Melgoza-Contreras71Sistemas Transdérmicos y Materiales Nanoestructurados, 2Toxicología y Genética, Universidad Nacional Autónoma de México, Cuautitlán Izcalli, México; 3Unidad de Enseñanza e Investigación, Hospital Regional de Alta Especialidad de Zumpango, Zumpango, México; 4Departamento de Ingeniería y Tecnología, 5Departamento de Ciencias Químicas, 6Laboratorio de Química Medicinal, Universidad Nacional Autónoma de México, Cuautitlán Izcalli, México; 7Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco, México City, MéxicoAbstract: Transdermal drug delivery offers an attractive alternative to the conventional drug-delivery methods of oral administration and injection. Apart from the convenience and noninvasiveness, the skin also provides a “reservoir” that sustains delivery over a period of days. It offers multiple sites to avoid local irritation and toxicity, yet it can also offer the option of concentrating drugs at local areas to avoid undesirable systemic effects. However, at present, the clinical use of transdermal delivery is limited by the fact that very few drugs can be delivered transdermally at a viable rate. This difficulty is because the stratum corneum of skin acts as an efficient barrier that limits penetration of drugs through the skin, and few noninvasive methods are known to significantly enhance the penetration of this barrier. In order to increase the range of drugs available for transdermal delivery, the use of nanocarriers has emerged as an interesting and valuable alternative for delivering lipophilic and hydrophilic drugs throughout the stratum corneum with the possibility of having a local or systemic effect for the treatment of many different diseases. These nanocarriers (nanoparticles, ethosomes, dendrimers, liposomes, etc) can be made of a lot of different materials, and they are very different in structure and chemical nature. They are too small to be detected by the immune system, and furthermore they can deliver the drug in the target organ using lower drug doses in order to reduce side effects.Keywords: skin, transdermal drug delivery, transdermal nanocarriers, nanoparticles, dendrimers, liposomes, nanoemulsions, transfersomes

Absorption and fluorescence spectral properties of hematoporphyrin in liposomes, micelles, and nanoparticles

Abstract A model photosensitizer, hematoporphyrin (Hp), encapsulated in various nanocarriers was investigated for both absorption and fluorescence properties. The generation of singlet oxygen upon light activation was also studied. The absorption intensity of nanoencapsulated hematoporphyrin was stronger and exhibited a red-shift of the Soret and Q absorption bands compared to the non-encapsulated hematoporphyrin. The fluorescence spectral changes were similar to the absorption spectral pattern. The generation of singlet oxygen for encapsulated hematoporphyrin upon light activation differed significantly from the free form hematoporphyrin, and the yield of singlet oxygen production was found in the following order: liposomes > micelles ≈ nanoparticles > free Hp. Under the current studied conditions, the use of nanocarriers significantly improve the photophysical properties of hematoporphyrin in aqueous solutions, and the liposome was the optimum system than either the micelle or the nanoparticle.

Therapy effects of gold nanorods on the CNE-1 nasopharyngeal carcinoma cell line

The use of nanocarriers to deliver drugs to tumor tissue is one of the most important strategies in cancer therapeutics. Recently, gold nanorods (GNRs) have begun to be used in cancer therapy because of their unique properties. The purpose of this study was to show the potential that GNRs have against human nasopharyngeal carcinoma CNE-1 cells, using near-infrared (NIR) laser light. Transmission electron microscopic and ultraviolet-visible spectroscopic investigations confirmed the efficient uptake of the GNRs by CNE-1 and human rhinal epithelia cells. The in vitro NIR photothermal therapy for the CNE-1 and rhinal epithelia cells was designed in three groups: (1) control, (2) laser alone, and (3) GNRs with laser. Fluorescence microscopy images indicated that, at some GNR concentrations and some intensities of NIR laser, GNRs with laser therapy could induce cell death for CNE-1 cells while keeping the rhinal epithelia cells healthy. Therefore, the results of this study suggest that using GNRs with NIR laser therapy can selectively destruct CNE-1 cells while having no effect on normal (rhinal epithelia) cells.

Photoinactivation of Staphylococcus epidermidis biofilms and suspensions by the hydrophobic photosensitizer curcumin – Effect of selected nanocarrier: Studies on curcumin and curcuminoides XLVII

Solubilization and stabilization from rapid degradation by the use of nanocarriers are necessary to exploit curcumin’s phototoxic potential towards pathogenic bacteria. However, maintenance of the phototoxicity requires a careful selection of type and amount of nanocarrier. The phototoxicity of an aqueous supersaturated curcumin solution without nanocarrier was compared to that of curcumin solubilized in polyethylene glycol 400 (PEG 400), Pluronic® F 127 (F 127) and hydroxypropyl-γ-cyclodextrin (HPγCD) on Staphylococcus (S.) epidermidis biofilms and suspensions. The nanocarriers stabilized the hydrophobic photosensitizer (PS) towards physical precipitation and hydrolytic degradation; however, photobleaching was pronounced (46–100% degradation) after irradiation with a dose of ∼9J/cm2 blue light depending on selected nanocarrier. Complete inactivation of S. epidermidis in suspension was achieved after exposure of ∼5J/cm2 combined with curcumin in 20% PEG 400 and 0.5% HPγCD and less than 1J/cm2 light in case of a supersaturated curcumin solution. Curcumin in 1.5% F 127 induced phototoxicity towards bacterial biofilms; however, it was not phototoxic towards planktonic S. epidermidis. All curcumin preparations investigated demonstrated significant and similar phototoxicity towards biofilms (13–29% bacterial survival). A ∼9J/cm2 light dose was not sufficient to eradicate S. epidermidis biofilm completely under the current conditions.

Influence of Molecular Size on the Retention of Polymeric Nanocarrier Diagnostic Agents in Breast Ducts

To investigate the influence of nanocarrier molecular size and shape on breast duct retention in normal rats using a non-invasive optical imaging method. Fluorescein-labeled PEG nanocarriers of different molecular weights and shapes (linear, two-arm, four-arm, and eight-arm) were intraductally administered (50nmol) to female Sprague-Dawley rats. Whole body images were obtained non-invasively. Fluorescence intensities (i.e., amount remaining in duct) were plotted against time to estimate the nanocarrier ductal retention half-lives (t(1/2)). Plasma samples were taken and the pharmacokinetics (Tmax, Cmax) of absorbed nanocarriers was also assessed. The t(1/2) of linear 12, 20, 30, 40, and two-arm 60kDa nanocarriers were 6.7 ± 0.9, 16.1 ± 4.1, 16.6 ± 3.4, 21.5 ± 2.7, and 19.5 ± 6.1h, whereas the four-arm 20, 40, and eight-arm 20kDa had t(1/2) of 9.0 ± 0.5, 11.5 ± 1.9, and 12.6 ± 3.0h. The t(1/2) of unconjugated fluorescein was significantly lower (14.5 ± 1.4min). The Tmax for 12, 40, 60kDa nanocarriers were 1, 24, and 32h, respectively, and only 30min for fluorescein. Since normal breast ducts are highly permeable, the use of nanocarriers may be helpful in prolonging ductal retention of diagnostic and/or therapeutic agents.

Phospho‐ibuprofen (MDC‐917) incorporated in nanocarriers: anti‐cancer activity in vitro and in vivo

Phospho-ibuprofen (P-I; MDC-917) inhibits the growth of colon cancer in mice. Here, we investigated the use of nanocarriers to improve its pharmacokinetics (PKs) and anti tumour efficacy. The cellular uptake and cytotoxicity of P-I encapsulated into liposomes and micelles, and its in vitro metabolic stability, were determined in cultures of human colon adenocarcinoma cells. The performance of liposomal P-I was further evaluated in PK studies in mice, and in a model of colon cancer xenografts in nude mice. Liposomal P-I and micellar P-I showed significantly enhanced cellular uptake in the colon cancer cells. Liposomal P-I also demonstrated increased cytotoxicity in vitro. Free P-I was metabolized rapidly to ibuprofen in the presence of purified esterases. In contrast, liposomal P-I, and to a lesser extent micellar P-I, was resistant to esterase-mediated hydrolysis. In mice, liposomal P-I partially protected P-I from hydrolysis in the circulation, and improved the biodistribution of intact P-I and its metabolites compared to free P-I. Liposomal P-I was more effective at inhibiting the growth of human colon cancer xenografts in mice, which may be explained on the basis of its improved PK profile compared to free P-I. Liposome encapsulation of P-I partially protected P-I from esterase-mediated hydrolysis in mice, enhanced the cytotoxicity and bioavailability of P-I and increased its efficacy at inhibiting the growth of human colon cancer xenografts. These results indicate that liposomes are suitable nanocarriers for the delivery of P-I, and that the anti-tumour potential of liposomal P-I merits further evaluation.

Enhanced transdermal permeability of estradiol using combination of PLGA nanoparticles system and iontophoresis

Estradiol is a therapeutic agent for treatment of perimenopausal symptoms and osteoporosis. Conventional oral or intravenous administration of estradiol has many problems, such as, metabolization in gastrointestinal tract and liver, pain by using an injection needle, rapid increase of drug levels in blood and fast clearance with unwanted side effects including thrombosis, endometriosis and uterus carcinoma. The use of nanocarriers for transdermal delivery has been studied because of their ability to deliver therapeutic agents for long time with a controlled ratio, escaping from the first pass effect by liver. In this study, permeability of estradiol-loaded PLGA nanoparticles through rat skin was studied. Higher amount of estradiol was delivered through skin when estradiol was loaded in nanoparticles than estradiol was free molecules. Also, iontophoresis was applied to enhance the permeability of nanoparticles. When iontophoresis was applied, permeability of estradiol-loaded PLGA nanoparticles was much higher than that obtained by simple diffusion of them through skin, since they have negative surface charges. They were found to penetrate through follicles mainly. Also, enhanced permeability effect of estradiol by using nanoparticle system and iontophoresis were observed in vivo. The combination of charged nanoparticle system with iontophoresis is useful for effective transdermal delivery of therapeutic agents.

Drug Targeting Strategies in Cancer Treatment: An Overview

Classic chemotherapy his little or no specificity for cancer cells, normally resulting in low accumulation at the tumor region (inefficacy), and in severe side effects (toxicity). This challenge has resulted in the development of several deliver strategies for chemotherapy agents to improve their concentration at the tumor site, simultaneously increasing their anticancer efficacy, while reducing the associated adverse systemic effects. In this work, the potential of drug delivery strategies involving the use of nanocarriers for controlling the biodistribution of antitumor drugs is deeply revised: passive targeting (through the enhanced permeability and retention effect, EPR effect) and active targeting (including stimuli-sensitive carriers and ligand-mediated delivery). Special attention will be also focussed on the recent approaches for overcoming multi-drug resistence. Finally, a general view of the problem of "nanotoxicity" in cancer treatment is also given.

Pulmonary Delivery: Innovative Approaches and Perspectives

The respiratory system, as well as the skin, are organs in direct contact with the environment and it they represent possible doors for the entrance of therapeutic agents into the body. Because of the increasing incidence of pulmonary diseases with high mortality and morbidity, pulmonary drug delivery is emerging as a non-invasive and attractive approach for the treatment of several pathologies. It must be pointed out that the development of drug delivery systems for pulmonary application requires a detailed knowledge of the lung, both in its healthy and disease state. Among the various drug delivery systems considered for pulmonary application, nanocarriers show several advantages over other conventional approaches for the treatment of respiratory diseases, for example prolonged drug release and cell-specific targeted drug delivery. Nano-size drug carriers can incorporate various therapeutics (e.g., poorly water soluble drugs, macromolecules) and show interesting features as drug delivery systems to the lung, such as: controlled release, protection from metabolism and degradation, decreased drug toxicity and targeting capabilities. Since gene therapy (e.g. small interfering RNA, siRNA) is currently being developed for a wide range of acute and chronic lung diseases, including CF, cancer and asthma, the use of nanocarriers for lung release/targeting represents a promising application of such nano-sized structures. Despite the many promising proof of concepts of various delivery technologies reported in this review, further efforts are needed to ensure the safety of long-term in vivo applications and the development of scale up from laboratory to industry in order to reach, together with safety, large - scale production at affordable costs of innovative lung delivery technologies.

Core-Cross-Linked Micelles Synthesized by Clicking Bifunctional Pt(IV) Anticancer Drugs to Isocyanates

Most low molecular weight platinum-based anticancer drugs have a short circulation time in the bloodstream. One of the potential strategies to improve the targeted delivery of cisplatin and prolong its circulation is via the use of nanocarriers. An improved drug delivery system was developed via reversible addition-fragmentation chain transfer (RAFT) polymerization. In a one-pot reaction, the incorporation of anticancer drug and core cross-linking was simultaneously carried out by using the highly effective reaction of isocyanate groups in the core of the polymeric micelles poly(oligo(ethylene glycol) methyl ether methacrylate)-block-poly(styrene-co-3-isopropenyl-α,α-dimethylbenzyl isocyanate) (POEGMA-block-P(STY-co-TMI)) with amine groups in the prepared platinum(IV) drug. The micelles with platinum(IV) incorporated with a size of 36 nm were very stable in water. In a reductive environment, in this study simulated using ascorbate, the drug was released at a slow rate of 82% in 22 days and at the same time the cross-linked micelle broke down into free block copolymers as evidenced using inductively coupled plasma-mass spectrometer (ICP-MS), size exclusion chromatography (SEC), and dynamic light scattering (DLS). The in vitro study also revealed the promising antitumor activity of prepared platinum(IV) drugs encapsulated into the micelle structure.

Progress in antiretroviral drug delivery using nanotechnology

There are currently a number of antiretroviral drugs that have been approved by the Food and Drug Administration for use in the treatment of human immunodeficiency virus (HIV). More recently, antiretrovirals are being evaluated in the clinic for prevention of HIV infection. Due to the challenging nature of treatment and prevention of this disease, the use of nanocarriers to achieve more efficient delivery of antiretroviral drugs has been studied. Various forms of nanocarriers, such as nanoparticles (polymeric, inorganic, and solid lipid), liposomes, polymeric micelles, dendrimers, cyclodextrins, and cell-based nanoformulations have been studied for delivery of drugs intended for HIV prevention or therapy. The aim of this review is to provide a summary of the application of nanocarrier systems to the delivery of anti-HIV drugs, specifically antiretrovirals. For anti-HIV drugs to be effective, adequate distribution to specific sites in the body must be achieved, and effective drug concentrations must be maintained at those sites for the required period of time. Nanocarriers provide a means to overcome cellular and anatomical barriers to drug delivery. Their application in the area of HIV prevention and therapy may lead to the development of more effective drug products for combating this pandemic disease.