Drug Delivery Agents Research Articles

MiRNA-520a-3p combined with folic acid conjugated Fe2O3@PDA multifunctional nanoagents for MR imagine and antitumor gene-photothermal therapy

Osteosarcoma (OS) is a primary malignant bone tumor that occurs mainly in adolescents. Researchers are devoting to develop combination therapy methods in a multifunctional nanoplatform for the treatment of osteosarcoma. The results of previous research have shown that up-regulation of miR-520a-3p could induce anticancer effects in osteosarcoma. In order to improve the effect of gene therapy (GT), we attempted to carry miR-520a-3p in a multifunctional vector for comprehensive therapy. Fe2O3 is a type of magnetic resonance imaging (MRI) contrast that is widely used as a drug delivery agent. When coated with polydopamine (PDA), it can also be used as a photothermal therapy (PTT) agent (Fe2O3@ PDA). To deliver nanoagents targeted to a tumor site, folic acid (FA) conjugated with Fe2O3 @PDA was manufactured as FA-Fe2O3@PDA. FA was chosen as the target molecule to enhance utilization and reduce toxicity of nanoparticles. However, the therapeutic efficacy of FA-Fe2O3-PDA combined with miR-520a-3p has not yet been studied. In this study, we synthesized FA-Fe2O3@PDA-miRNA and investigated the potential of combining PDA regulated PTT and miR-520a-3p regulated GT to kill osteosarcoma cells. The results indicated that down-regulation of interleukin 6 receptor (IL6R) by miR-520a-3p and the photothermal ability of PDA could induce satisfactory anticancer effects in osteosarcoma, and the curative ratio was better than that used alone PTT or GT. Moreover, as a kind of T 2 magnetic contrast, miRNA-Fe2O3@PDA-FA can be used for MRI. These findings indicated that miRNA-Fe2O3@PDA-FA is an effective anti-tumor nanovector for PTT combined with GT.

Functionalized europium-doped hollow mesoporous silica nanospheres as a cell imaging and drug delivery agents

In an effort to enhance the antitumor efficacy of breast cancer treatment, the chemotherapeutic agent Paclitaxel (PTX) was encapsulated within hyaluronic acid (HA) modified hollow mesoporous silica (HMSNs). In vitro drug release assays showed that the resulting formulation, Eu-HMSNs-HA-PTX, exhibited enzyme-responsive drug release. In addition, cell cytotoxicity and hemolysis assays demonstrated the favorable biocompatibility of both Eu-HMSNs and Eu-HMSNs-HA. Notably, compared to Eu-HMSNs alone, Eu-HMSNs-HA showed enhanced accumulation within CD44-expressing cancer cells (MDA-MB-231). As anticipated, apoptosis experiments indicated that Eu-HMSNs-HA-PTX displayed significantly greater cytotoxicity toward MDA-MB-231 cells than non-targeted Eu-HMSNs-PTX and free PTX. In conclusion, Eu-HMSNs-HA-PTX demonstrated excellent anticancer effects and holds promise as a potent candidate for the efficient therapy of breast cancer.

Novel fluorescein isothiocyanate (FITC) cored PAMAM dendrimers as drug delivery agent

Fluorescent dyes, or fluorophores, enable researchers to visualize specific biological molecules by fluorescence microscopy. Herein, a novel fluorescent FITC-poly(amidoamine) (FITC-PAMAM) dendrimers have been synthesized via divergent approach. The molecular structure of the FITC-PAMAM dendrimers (G-0 to G5) was characterized by 1H NMR, 13C NMR spectroscopy and by FTIR. In order to emphasize the structural efficacy of FITC-PAMAM dendrimer, the drug delivery behavior has been evaluated by using 5-fluorouracil (5-FU) as a model cancer therapy drug. Anti-proliferative activity of FITC-cored PAMAM dendrimers in all generations (G0-G5) with or without 5-FU were analyzed on human gastric carcinoma cells (AGS) by WST-1 cell proliferation assay. Initially, the nontoxic dose of unloaded FITC-PAMAM dendrimers was assessed for further drug loading experiments. Loading of 5-FU into FITC-PAMAM dendrimers, regardless of generation, increased the toxicity of the drug. Besides, 5-FU loaded FITC-PAMAM dendrimers induced a generation-based gradual inhibition of cell proliferation. FITC and phase contrast merged images indicated that FITC-PAMAM dendrimers facilitate the entry of the drug into the cells, in a generation-dependent manner. The FITC- dendrimers may serve as a promising intracellular drug delivery agent for 5-FU by increasing cell uptake into cells and thereby, enhancing antiproliferative activity on AGS cells in a generation-dependent manner.

Platelet concentrates – A panacea for periodontal regeneration.

Periodontitis is an inflammatory condition of the periodontium leading to loss of supporting structures of the tooth. The regeneration of periodontium refers to the restoration of the lost tissues to their original form and function by reiterating the fundamental wound healing processes involved in their development. Research has led to the development of “Autologous biomaterials” provide signals for healing, repair, and regeneration. These autologous substances also fosters neo-angiogenesis and new bone formation and therefore have yielded encouraging results in the field of regenerative dentistry. Platelet concentrates have higher concentration of growth factors which enhance periodontal regeneration. Blood derivatives have several advantages such as being autogenous, cost effective, less time consuming, simple to perform and prolonged release of growth factors. Since inception, many approaches have evolved also in-depth research has been done regarding its biological and clinical applications. Several modifications have been advocated in the conventional protocol like the advanced PRF, injectable PRF, PRF lysate and Titanium-prepared PRF. This review paper addresses the evolution, applications of platelet concentrates for tissue engineering, recent advances, and novel protocols. Furthermore, several future perspectives of platelet concentrates, such as platelet concentrates as drug delivery agents, platelet dust and liposomes encapsulating platelet concentrates are also discussed.

Synthesis and Characterization of Hydrogel Alginate/Poly (N-Vinyl -2-Pyrrolidone) with Double Ionic Cross-Bonded for Drug Delivery and Antibacterial Agent

Synthesis and Characterization of Hydrogel Alginate/Poly (N-Vinyl -2-Pyrrolidone) with Double Ionic Cross-Bonded for Drug Delivery and Antibacterial Agent

Fe3O4 Core–Shell Nanostructures with Anticancer and Antibacterial Properties: A Mini-Review

Core–shell nanoparticles are functional materials with tailored properties, able to improve the requirements of various applications. Both core and shell components can be inorganic or organic, and there are numerous studies in this field regarding their synthesis methods, properties, and applications. This review aims to study core–shell nanostructures with Fe3O4 cores and different shell types, observing their antibacterial and anticancer properties. By the type of coating, Fe3O4 core–shell nanoparticles (NPs) are classified into four categories: metal-coated NPs, metal-organic framework (MOF) coated NPs, metal oxide coated NPs, and polymer-coated NPs. Each category is briefly presented, emphasizing anticancer or antibacterial properties and specific applications (cancer diagnosis or therapy, drug carrier). Moreover, synthesis methods and particle size for both core and shell nanostructures, as well as the magnetic properties of the final core–shell material, are summarized in this review. Most of the consulted papers discussed sphere-like core–shell nanoparticles obtained by chemical methods such as coprecipitation, hydrothermal, and green synthesis methods using plant extract. These types of core–shell nanoparticles could be used as drug nanocarriers for tumor-targeted drug delivery, hyperthermia treatment, or contrast agents. Further work needs to be conducted to understand nanoparticles’ interaction with living cells and their traceability in the human body.

Photocatalytic Metal‐Free Radical Hydrosilylation for Polymer Functionalization†

Comprehensive SummaryPost‐modification of polymers offers a route to prepare functionalized polymers through efficient chemical reactions, and hydrosilylation is one of the most effective strategies. Silane‐functionalized polymers have found a wide range of potential applications, such as adhesives, rubbers, and drug delivery agents. For decades, the hydrosilylation for the post‐modification of polymers has typically used transition metals as catalysts. Metal‐free hydrosilylation strategies that can avoid metal residues in polymers are largely lacking in this field. Herein, we report the photocatalytic metal‐free radical hydrosilylation strategy for the post‐modification of polymers bearing pendant vinyl groups using the organic photocatalyst and hydrogen atom transfer (HAT) catalyst under blue light irradiation. We used monofunctional silanes to functionalize polymers and the bis(silane)s as crosslinkers to prepare crosslinked polymers.

Biocompatible polysaccharide fabricated graphene oxide nanoparticles: A versatile nanodrug carrier to deliver κ- carrageenan against cancer cells

A graphene oxide mediated hybrid nano system for pH stimuli-responsive and in vitro drug delivery targeted for cancer was described in this study. Graphene oxide (GO) functionalized Chitosan (CS) mediated nanocarrier capped with xyloglucan (XG) was fabricated with and without Kappa carrageenan (κ-C) from red seaweed, Kappaphycus alverzii, as an active drug. FTIR, EDAX, XPS, XRD, SEM and HR-TEM studies were carried out for GO-CS-XG nanocarrier loaded with and without active drugs to understand the physicochemical properties. XPS (C1s, N1s and O1s) confirmed the fabrications of XG and functionalization of GO by CS via the binding energies at 284.2 eV, 399.4 eV and 531.3 eV, respectively. The amount of drug loaded in vitro was 0.422 mg/mL. The GO-CS-XG nanocarrier showed a cumulative drug release of 77 % at acidic pH 5.3. In contrast to physiological conditions, the release rate of κ-C from the GO-CS-XG nanocarrier was considerably higher in the acidic condition. Thus, a pH stimuli-responsive anticancer drug release was successfully achieved with the GO-CS-XG-κ-C nanocarrier system for the first time. The drug release mechanism was carried out using various kinetic models that showed a mixed release behavior depending on concentration and diffusion/swelling mechanism. The best-fitting model which supports our release mechanism are zero order, first order and Higuchi models. GO-CS-XG and κ-C loaded nanocarrier biocompatibility were determined by in vitro hemolysis and membrane stabilization studies. MCF-7 and U937 cancer cell lines were used to study the cytotoxicity of the nanocarrier by MTT assay, which indicates excellent cytocompatibility. These findings support the versatile use of a green renewable biocompatible GO-CS-XG nanocarrier as targeted drug delivery and potential anticancer agent for therapeutic purposes.

Nano Drug Delivery Systems: A Mini-review

Abstract: Medical nanotechnology is surfacing as a challenging arena covering new biomedical applications, such as drug delivery, treatment, nano diagnosis, controlled drug release, regenerative medicine, and disease prevention. The recent developments in the field of Nanotechnology have enabled the nanostructures to overcome the problems associated with drug delivery making them the promising agents for site-specific drug delivery with reduced side effects and the best treatment outcome. These nanodrug delivery systems are designed in such a way that they can breach the biological barrier and deliver the drug in a site-specific manner. They enhance the effectiveness of drugs by increasing the stability and water solubility of drugs and by increasing the rate at which these nano drug complexes are taken up by the cells and tissues. Dendrimers, nanocrystals, nano-polymer NPs, and liposomes are futuristic nano-based drug delivery systems. Smart polymers are future drug-delivery systems with cutting-edge precise technology that are employed in effective cellular targeting based on temperature, pH, photoresponsive, conductive and magnetic responsive smart polymers. This review provides a comprehensive view of various nanostructures and their application in drug delivery.

Toehold-Mediated Shape Transition of Nucleic Acid Nanoparticles.

We introduce a toehold-mediated strand displacement strategy for regulated shape-switching of nucleic acid nanoparticles (NANPs) enabling their sequential transformation from triangular to hexagonal architectures at isothermal conditions. The successful shape transitions were confirmed by electrophoretic mobility shift assays, atomic force microscopy, and dynamic light scattering. Furthermore, implementation of split fluorogenic aptamers allowed for monitoring the individual transitions in real time. Three distinct RNA aptamers─malachite green (MG), broccoli, and mango─were embedded within NANPs as reporter domains to confirm shape transitions. While MG "lights up" within the square, pentagonal, and hexagonal constructs, the broccoli is activated only upon formation of pentagon and hexagon NANPs, and mango reports only the presence of hexagons. Moreover, the designed RNA fluorogenic platform can be employed to construct a logic gate that performs an AND operation with three single-stranded RNA inputs by implementing a non-sequential polygon transformation approach. Importantly, the polygonal scaffolds displayed promising potential as drug delivery agents and biosensors. All polygons exhibited effective cellular internalization followed by specific gene silencing when decorated with fluorophores and RNAi inducers. This work offers a new perspective for the design of toehold-mediated shape-switching nanodevices to activate different light-up aptamers for the development of biosensors, logic gates, and therapeutic devices in the nucleic acid nanotechnology.

DFT study of D-Penicillamine adsorption on Al and Ga doped boron nitride (Al-B11N12 and Ga-B11N12) nanoclusters as drug delivery agents

A comprehensive computational investigation was performed in this study on the adsorption of a penicillamine (PCA) molecule as drug onto Al- and Ga-doped B12N12 nanoclusters in aqueous and chloroform environments, using density functional theory calculations. The main aim was to evaluate the capability of the nanocluster in drug delivery applications. The PCA molecule interacts effectively with Al- and Ga-doped clusters via its four nucleophilic sites: amine, carbonyl, hydroxyl, and thiol. Using the computational results, the most stable adsorption complexes were obtained when the PCA molecule adsorbs through its amine group with −4.75 and −4.67 eV adsorption energies for Al-B11N12 and Ga-B11N12 nanocages, respectively. The adsorption of the PCA molecule decreases the HOMO–LUMO gaps and the global hardness of the doped clusters, which corroborated increases in reactivity of the considered clusters for drug delivery purpose. Our computational studies exhibit that Al and Ga atoms doping improves the drug delivery capacity of B12N12 nanoclusters.

PHYTO-SYNTHESIS OF GOLD NANOPARTICLES USING Trewia nudiflora FRUIT EXTRACT WITH HAuCl4, CHARACTERIZATION, EVALUATION, AND ANTIMICROBIAL ACTIVITIES

Due to their excellent catalytic, good biocompatibility, large surface area, conductivity, drug delivery agent, and antimicrobial activity properties, nanoparticles with medicinal plants are great for biomedical applications. The study was conducted from January 2017 to October 2018 at the Department of Applied Nutrition and Food Technology, Islamic University, Kushtia. The main aim of this study was to synthesize, characterize, and evaluate the antimicrobial activity of gold nanoparticles using the fruit of Trewia nudiflora as a primary source. Phyto-constituents of Trewia nudiflora were extracted with water to synthesize gold nanoparticles (AuNPs). There was a ratio of chloroauric acid (HAuCl4) solution and Trewia nudiflora fruit extract (20:1) used to optimize gold nanoparticles (AuNPs), respectively. Synthesized gold nanoparticles were confirmed by a visual color change from colorless to ruby-red, Laser beam light was passing through the synthesized gold nanoparticles to observe the Tyndall effect. UV-Vis spectroscopy was used to observe the absorption peaks between 500 and 550 nm, which is the characteristic peak range for gold nanoparticles (AuNPs). The surface morphology of the AuNPs was examined by scanning electron microscopy (SEM) and the elemental composition of the sample (AuNPs) by energy-dispersive X-ray analysis (EDAX). The antimicrobial activity of gold nanoparticles was observed in an 8.5-mm zone of inhibition against gram negative (Klebsiella sp.) and 8-mm zone of inhibition against gram positive (Micrococcus sp.) bacteria.

DNA interactive property of poly-L-lysine induces apoptosis in MCF-7 cells through DNA interaction.

Poly-L-lysine(PLL)is known to be an encapsulating agent in drug formulation and delivery. PLL also has apoptotic and antiproliferative activities that enable blocking of the tumorigenesis process. However, the dose-selective activities of PLL in exerting apoptosis against cancer are unclear. Therefore, this study has been designed to explore the potential role and dose of PLL in apoptosis, if any. For this, PLL was administered at several doses in cancer cell lines and was found to be more potent against MCF-7 cells. PLL causes mitochondria-mediated apoptotic death through the upregulation of cleaved caspase-3. To investigate the mechanism responsible for this activity, we have analyzed if PLL could have the DNA interactive property or not. For this, molecular docking analysis was carried out to prove whether it has the property to bind with DNA or not. Studies have revealed that PLL is a potent DNA binder and it probably performs such apoptotic activities through the binding of cellular DNA early in an exposure. Simultaneous upregulation of both ROS-mediated stress and also in key protein expressions likeγ-H2AX could also help us to confirm that PLL induces apoptosis through DNA interaction. This finding leads us to believe that PLL could play an interfering role with other chemotherapeutic compounds when used as a drug-coating material as it exerts an apoptotic effect on cancer cells, which should be avoided by using a much lower concentration.

Metal–organic frameworks in diagnostics, therapeutics, and other biomedical applications

AbstractMetal–organic frameworks (MOFs) are emerging porous coordination polymers constructed by metal ions and organic linkers that have attracted numerous interests in recent years. The large surface area, high porosity, tunable size, and versatile functionality make them promising materials for cargo delivery (i.e., drugs, mRNA, dyes) and sensing (i.e., nucleic acids, small molecules, ions). In addition, the metal ions released from MOFs offer antibacterial and antifungal utility. This review presents a snapshot of current MOF‐related research, highlighting the synthesis approaches, and the various bioapplications of MOFs in terms of biosensing platforms, drug delivery, and antimicrobial agents, exposing potential for future research in the MOF field.

Size and Morphology-Mediated Antiproliferative Activity of Hydroxyapatite Nanoparticles in Human Breast Cancer Cells

Hydroxyapatite nanoparticles (nHAPs) have been recognized for potent antitumor effects in certain cancer cells, making them good candidates as drug delivery agents and tumor therapeutics with fewer than normal side effects. This study is aimed to correlate cell proliferation inhibition with the size and morphology of nHAPs in a human breast cancer cell line as well as in normal tissue cells. We present our in vitro experimental evidence that nHAPs with sizes smaller than 50 nm have high inhibitory activity against human MCF-7 breast cancer cell lines. Based on our experimental data, normal fibroblast cells (NIH 3T3) were relatively more viable upon treatment with the nanoconstructs. The present study indicates that nHAPs can be engineered as nontoxic specific inhibitors as efficient breast cancer therapeutics in humans.

A Novel Approach for Enhanced Osteosarcoma Photodynamic Therapy Using Encapsulated Methylene Blue in Silica Nanoparticles

Photodynamic therapy (PDT) is a cutting-edge cancer treatment that utilizes both light and photosensitizers (PSs) to attack cancer cells. Methylene blue (MB) has emerged as a highly promising photosensitizer (PS) in PDT therapy due to its exceptional ability to produce singlet oxygen, which is attributed to its high quantum yield. However, the main challenge in utilizing MB in photodynamic therapy is its effective delivery to the target tissue. This challenge can be addressed by utilizing silica nanoparticles (SiNPs) as a drug delivery agent. Silica nanoparticles encapsulate MB and prevent its leakage, offering a novel approach to improving PDT therapy by reducing the toxicity of MB and increasing its bioavailability at the target cell. In this study, an extensive analysis of the size and shape evolution of the synthesized silica nanoparticles loaded with MB was conducted using TEM. Various encapsulated and bare MB concentrations were tested for cytotoxicity against osteosarcoma cells. Moreover, the optimal concentration and exposure time under light (with an intensity of approximately 8.9 mW/cm2 in the visible range) were determined to achieve maximum cell elimination. The results revealed that encapsulated MB in SiNPs exhibited a higher efficacy compared to naked MB, with a 50% increase in concentration effectiveness and a 90% increase in exposure time efficacy. This confirms that encapsulated MB in SiNPs is more effective in killing osteosarcoma cells than bare MB, thereby enhancing photodynamic therapy through increased bioavailability of MB in target cells. The enhanced bioavailability of MB in target cells as a result of its encapsulation in SiNPs makes it a highly promising drug delivery candidate for significantly enhancing the efficacy of photodynamic therapy against osteosarcomas.

Mechanistic Understanding of Protein Corona Formation around Nanoparticles: Old Puzzles and New Insights.

Although a wide variety of nanoparticles (NPs) have been engineered for use as disease markers or drug delivery agents, the number of nanomedicines in clinical use has hitherto remained small. A key obstacle in nanomedicine development is the lack of a deep mechanistic understanding of NP interactions in the bio-environment. Here, the focus is on the biomolecular adsorption layer (protein corona), which quickly enshrouds a pristine NP exposed to a biofluid and modifies the way the NP interacts with the bio-environment. After a brief introduction of NPs for nanomedicine, proteins, and their mutual interactions, research aimed at addressing fundamental properties of the protein corona, specifically its mono-/multilayer structure, reversibility and irreversibility, time dependence, as well as its role in NP agglomeration, is critically reviewed. It becomes quite evident that the knowledge of the protein corona is still fragmented, and conflicting results on fundamental issues call for further mechanistic studies. The article concludes with a discussion of future research directions that should be taken to advance the understanding of the protein corona around NPs. This knowledge will provide NP developers with the predictive power to account for these interactions in the design of efficacious nanomedicines.

Review of Zinc Oxide Nanoparticles: Toxicokinetics, Tissue Distribution for Various Exposure Routes, Toxicological Effects, Toxicity Mechanism in Mammals, and an Approach for Toxicity Reduction.

Zinc oxide (ZnO) nanoparticles (NPs) are widely used as a sunscreen, antibacterial agent, dietary supplement, food additive, and semiconductor material. This review summarizes the biological fate following various exposure routes, toxicological effects, and toxicity mechanism of ZnO NPs in mammals. Furthermore, an approach to reduce the toxicity and biomedical applications of ZnO NPs are discussed. ZnO NPs are mainly absorbed as Zn2+ and partially as particles. Regardless of exposure route, elevated Zn concentration in the liver, kidney, lungs, and spleen are observed following ZnO NP exposure, and these are the target organs for ZnO NPs. The liver is the main organ responsible for ZnO NP metabolism and the NPs are mainly excreted in feces and partly in urine. ZnO NPs induce liver damage (oral, intraperitoneal, intravenous, and intratracheal exposure), kidney damage (oral, intraperitoneal, and intravenous exposure) and lung injury (airway exposure). Reactive oxygen species (ROS) generation and induction of oxidative stress may be a major toxicological mechanism for ZnO NPs. ROS are generated by both excess Zn ion release and the particulate effect resulting from the semiconductor or electronic properties of ZnO NPs. ZnO NP toxicity can be reduced by coating their surface with silica, which prevents Zn2+ release and ROS generation. Due to their superior characteristics, ZnO NPs are expected to be used for biomedical applications, such as bioimaging, drug delivery, and anticancer agents, and surface coatings and modification will expand the biomedical applications of ZnO NPs further.

Synthesis of Thiolated Cashew Gum and Its Evaluation as an Improved Mucoadhesive Agent in Drug Delivery

The objectives of present research work were to extract cashew exudate gum (CG), perform thiolation of extracted CG, and evaluate the synthesized thiolated cashew exudate gum (TCG) as a mucoadhesive agent in designing metronidazole mucoadhesive gels and metronidazole mucoadhesive buccal discs. The CG was thiolated or thiol-modifi ed via esterifi cation utilizing thioglycolic acid and hydrochloric acid. Metronidazole mucoadhesive gels and metronidazole mucoadhesive buccal discs made of unmodifi ed CG and TCG (as mucoadhesive agent) were formulated and evaluated to reveal their bio-mucoadhesive potentials in drug delivery. The yield of thiolated product (TCG) was 56.24%, and the thiol-group content in TCG was found to be 9.06 mM of thiol group/g of CG. FTIR analysis indicated the thiolation of CG in the synthesized TCG. Both types of formulations (mucoadhesive gels and buccal discs) made of TCG exhibited excellent improved ex-vivo bio-mucoadhesion and consistent pattern of metronidazole releasing over a prolonged time. The synthesized TCG can be utilized as an improved mucoadhesive material in designing bio-mucoadhesive systems for drug delivery.

Increased efficacy of biologics following inhibition of autophagy in A549 lung cancer cells in bimodal treatment of doxorubicin and SAR405-loaded chitosan nanoparticles

Conventional anti-cancer drugs, including doxorubicin, are associated with high toxicity and non-specific distribution in the body which results in a cascade of side effects. Cancer cells can utilize autophagy to promote tolerance to the stress induced by anti-cancer agents; this may be the major cause of drug resistance in advanced tumors. Owing to the molecular dynamism of cancer cells, targeting the pro-apoptotic survival pathways such as autophagy may increase the effectiveness of existing therapeutic agents at lower concentrations, thereby reducing the side effects of such agents. SAR405 is an inhibitor of autophagy activity due to its molecular interactions within the ATP binding site; however, it suffers from extracellular premature degradation and poor cellular uptake. Conversely, chitosan nanoparticles are considered biologically degradable, non-toxic, and biocompatible drug delivery agents that can be used to minimize the side effects of conventional therapeutic agents whilst increasing their intracellular uptake. In this study, a binary therapeutic strategy for the enhancement of the efficacy of doxorubicin while simultaneously inhibiting autophagy via a nano-mediated delivery system is reported. Autophagic inhibition was achieved via the improvement of SAR405 cellular uptake using SAR405-loaded chitosan nanoparticles. The synthesized nanoparticles were subsequently characterized for parameters of hydrodynamic diameter and polydispersity, while encapsulation and drug loading efficiencies were determined. Morphological characterization of the nanoparticles was elucidated using electron microscopy, and the cytotoxicity of the SAR405-loaded chitosan nanoparticles in combination treatments with doxorubicin was assessed through MTT and Annexin-v apoptosis assays. Autophagy progression through autophagosome formation was also evaluated using CYTO-ID staining. Following encapsulation, the size of the SAR405-loaded chitosan nanoparticles significantly increased from 54 nm to 161 nm at 10 µM SAR405 concentration, while the polydispersity index increased from 0.11 to 0.31 denoting presence of both encapsulated and unencapsulated moieties. When A549 lung cancer cells were treated with the IC50 values of doxorubicin in combination with SAR405-encapsulated CNP, an approximately 47% more reduction in cell viability was observed via the Annexin V-FITC/PI assay compared to using doxorubicin alone. Inhibition of autophagy was also detected in cells treated with SAR405 delivered using the nanoparticle system and was thought to be the primary reason towards a decrease in the resistance of the cancer cells to doxorubicin and thus increased its efficacy at lower concentrations. Therefore, this study has demonstrated a potential way of targeting cancer cell survival pathways that can be considered an effective way of increasing the efficacy of chemotherapeutic drugs.