Controlled Drug Release Properties Research Articles

High-amylose sodium carboxymethyl starch matrices: development and characterization of tramadol hydrochloride sustained-release tablets for oral administration.

Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100 mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol.

PH-responsive nanofibers with controlled drug release properties

Smart polymers and nanofibers are potentially intriguing materials for controlled release of bioactive agents. This work describes a new class of pH responsive nanofibers for drug delivery systems with controlled release properties. Initially, poly(4-vinylbenzoic acid-co-(ar-vinylbenzyl)trimethylammonium chloride) [poly(VBA-co-VBTAC)] was synthesized via reversible addition–fragmentation chain transfer (RAFT) polymerization. Then, ciprofloxacin was chosen as the model drug for the release study and encapsulated into pH-responsive polymeric carriers of poly(VBA-co-VBTAC) nanofibers via electrospinning. The morphology of the electrospun nanofibers was examined by scanning electron microscopy (SEM). The structural characteristics of the pH responsive nanofibers were investigated by Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD). The release measurements of ciprofloxacin from pH responsive nanofibers were also performed by high-performance liquid chromatography (HPLC) analysis. To show the pH sensitivity of these nanofibers, the release profile of ciprofloxacin was examined under acidic, neutral and basic conditions. The results indicate that pH responsive nanofibers can serve as effective drug carriers since the release of ciprofloxacin could be controlled by changing the pH of the environment, and therefore these drug loaded pH-responsive nanofibers might have potential applications in the biomedical field.

Design and Synthesis of Lipidic Organoalkoxysilanes for the Self‐Assembly of Liposomal Nanohybrid Cerasomes with Controlled Drug Release Properties

This paper reports the facile design and synthesis of a series of lipidic organoalkoxysilanes with different numbers of triethoxysilane headgroups and hydrophobic alkyl chains linked by glycerol and pentaerythritol for the construction of cerasomes with regulated surface siloxane density and controlled release behavior. It was found that the number of triethoxysilane headgroups affected the properties of the cerasomes for encapsulation efficiency, drug loading capacity, and release behavior. For both water-soluble doxorubicin (DOX) and water-insoluble paclitaxel (PTX), the release rate from the cerasomes decreased as the number of triethoxysilane headgroups increased. The slower release rate from the cerasomes was attributed to the higher density of the siloxane network on the surface of the cerasomes, which blocks the drug release channels. In contrast to the release results with DOX, the introduction of one more hydrophobic alkyl chain into the cerasome-forming lipid resulted in a slower release rate of PTX from the cerasomes due to the formation of a more compact cerasome bilayer. An MTT viability assay showed that all of these drug-loaded cerasomes inhibited proliferation of the HepG2 cancer cell line. The fine tuning of the chemical structure of the cerasome-forming lipids would foster a new strategy to precisely regulate the release rate of drugs from cerasomes.

Targeted, Monitored, and Controlled Chemotherapy: A Multimodal Nanotechnology-Based Approach against Cancer

We review innovative methods for treatment of cancer tumor on the basis of nanotechnology and physics to target, monitor and control release of chemotherapeutic agents. Chemotherapy is one of the main methods of treatment for cancer and plays a vital role in clinical practice, but side effects of anticancer drugs are still critical problems. Magnetic nanoparticles can be applied as an effective drug carriers and contrast agents for magnetic resonance imaging (MRI). Since certain nanoparticles have magnetic properties, they can be trapped in tumor during blood circulation by an external magnetic field. Also, polymeric nanoparticles are great candidates to encapsulate anticancer drugs and to control the release profile of drugs in biologic media. We suggest the construction of drug-loaded polymer-coated magnetic (DPM) nanoplatform with the potential for being utilized in medical imaging as well as having controlled drug release properties. Nanoplatform distribution can be monitored by MRI and with clever combination of ultrasound physics and suggested DPM nanoplatform, it would be feasible to increase the rate of drug release (in situ) and drug uptake by cancerous cell. To optimize the level of drug uptake by cancerous cell, the selection of ultrasound frequency and intensity is essential. The development of suggested method could be a new approach against cancer tumor.

PH-sensitive IPN hydrogel based on poly (aspartic acid) and poly (vinyl alcohol) for controlled release

Various pH-sensitive sequential interpenetrating polymer network (IPN) hydrogels were prepared by introducing poly (vinyl alcohol) (PVA) hydrogel into Poly (aspartic acid) (PASP) hydrogel by freeze-thawing treatment to obtain a novel drug delivery system to the intestine. The structure and the morphologies of the prepared hydrogels were studied by Fourier Transform Infrared Spectroscopy (FTIR) and scanning electron microscopy (SEM). The thermal behavior and crystallinity of the hydrogels were characterized by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). Their pH-sensitive properties moreover were studied and the results revealed that both PASP hydrogel and IPN hydrogels exhibited excellent pH-sensitivity. Furthermore, the controlled drug release properties of the hydrogels were also evaluated and results indicated that by increasing the PVA fraction in the IPN hydrogel, the release of Naproxen sodium was improved. These results show that the IPN hydrogels could be a suitable carrier for site-specific drug delivery in the intestine.

Thermo-responsive hollow silica microgels with controlled drug release properties

Thermo-responsive hollow silica microgels (THSMGs) consisting of a hollow core, an intermediate silica supporting layer and a smart polymer gel corona were fabricated via organic–inorganic hybridization. Hollow silica particles and PNIPAAm microgels were successfully combined by utilizing the cross-linking reaction between 3-(trimethoxysilyl) propyl methacrylate (TMSPMA) and silanol groups on the silica surface, and then the copolymerization of TMSPMA and N-isopropylacrylamide (NIPAAm). The morphology and chemical composition were systematically examined by field emission scanning electron microscope (FESEM), transmission electron microscope (TEM), energy dispersive X-ray spectroscopy (EDS) and the Brunauer–Emmett–Teller (BET) measurement. The thermo-responsive phase transition behavior was investigated by the determination of the lower critical solution temperature (LCST), and particle size measurement using dynamic light scattering. THSMGs remain porous even after the coverage of PNIPAAm gels, and also have obvious hydrophilic/hydrophobic transition property and good swelling/collapse capability in spite of the rigid silica layer. The results of in vitro cytotoxicity evaluation and Rhodamine B (RHB) release study demonstrated that THSMGs have good biocompatibility, and achieve a thermo-responsive controlled-release behavior. The prepared THSMGs show considerable potential for applications as targeted and ambient temperature responsive drug delivery system.

Preparation and characterization of minoxidil loaded nanostructured lipid carrier gel for effective treatment of alopecia

In the present work attempts have been made to prepare the nanostructured lipid carrier (NLC) gel, by using minoxidil, which is preferably used in case of Alopecia, i.e. baldness pattern as a effective drug. The nine different formulations of Minoxidil-NLC (NLC1–NLC9) were prepared using solid and liquid lipids with Cholesterol and Soya lecithin in different concentrations by the melt dispersion ultrasonication method. Properties of NLC1–NLC9 such as the particle size and its distribution, the scanning electron microscopy (SEM), the drug entrapment efficiency (EE), and the drug release behavior were investigated. The nanoparticulate dispersion was suitably gelled and characterized with respect to drug content, pH, spreadability, rheology, and in vitro release. Safety of the NLC-based gel was assessed using primary skin irritation studies. The formulated NLC3 was spherical in shape, with average particle size of 280nm, zeta potential of −42.40mV and entrapment efficiency of 86.09%. Differential Scanning Calorimeter (DSC) measurements revealed that imperfect crystallization occurred in the inner core of the NLC particles. The drug release behavior from the NLC displayed a biphasic drug release pattern with burst release at the initial stage followed by sustained release. These results indicated that the NLC3 is a suitable carrier of minoxidil with improved drug loading capacity and controlled drug release properties. It has been observed that NLC gel produces the gel with good consistency, homogeneity, spreadability and rheological behavior. The developed NLC-based gel showed faster onset and elicited prolonged activity up to 16h. The present study concluded that the NLC-based gel containing minoxidil dissolved in a mixture of solid lipid and liquid lipid in the nanoparticulate form helped us to attain the objective of faster onset yet prolonged action as evident from in vitro release.

A facile preparation of targetable pH-sensitive polymeric nanocarriers with encapsulated magnetic nanoparticles for controlled drug release

Novel multifunctional nanocomposites were successfully prepared for the controlled release of anti-cancer drug and magnetic resonance imaging (MRI) via a simple self-assembly process. In this strategy, superparamagnetic iron oxide nanoparticles (SPIONPs) were “fixed” between the hydrophobic segment of the pH-sensitive amphiphilic polymer (HAMAFA-b-DBAM) and the surface of hollow mesoporous silica nanoparticles (HMS) which were modified by the long-chain hydrocarbon octadecyltrimethoxysilane (C18). Since the amphiphilic polymer was conjugated with a folic acid (FA) group, the nanocomposites could target the folic acid receptor (FR) of over-expressed tumor cells efficiently. Moreover, high drug loading content was obtained simultaneously due to the hollow core of HMS. The loaded drug could release from the HMS core triggered by the mildly acidic pH environment in the cancer cells due to the hydrolysis of the pH-sensitive polymer shell. The targeting process of the nanocomposites could be easily tracked by MRI due to the magnetism of the SPIONPs. Therefore, a nanocarrier with high drug-loading capacity and controlled drug release property for tumor diagnosis and therapy was obtained via the self-assembly of HMS core, magnetic Fe3O4 nanoparticles and targetable pH-sensitive polymer shell.

Zeolitic imidazolate framework-8 as efficient pH-sensitive drug delivery vehicle

Zeolitic Imidazolate Framework-8 (ZIF-8), for the first time for ZIFs, exhibits a remarkable capacity for the anticancer drug 5-fluorouracil (5-FU), around 660 mg of 5-FU/g of ZIF-8, and presents a pH-triggered controlled drug release property. These prove ZIF-8 to be a valuable candidate for delivery of anticancer agents and reveal its potential applications in the treatment of cancer.

Mechanisms of burst release from pH-responsive polymeric microparticles

Microencapsulation of drugs into preformed polymers is commonly achieved through solvent evaporation techniques or spray drying. We compared these encapsulation methods in terms of controlled drug release properties of prepared microparticles and investigated the underlying mechanisms responsible for the 'burst release' effect. Using two different pH-responsive polymers with a dissolution threshold of pH 6 (Eudragit L100 and AQOAT AS-MG), hydrocortisone, a model hydrophobic drug, was incorporated into microparticles below and above its solubility within the polymer matrix. Although, spray drying was an attractive approach due to rapid particle production and relatively low solvent waste, the oil-in-oil microencapsulation method was superior in terms of controlled drug release properties from the microparticles. Slow solvent evaporation during the oil-in-oil emulsification process allowed adequate time for drug and polymer redistribution in the microparticles and reduced uncontrolled drug burst release. Electron microscopy showed that this slower manufacturing procedure generated nonporous particles whereas thermal analysis and X-ray diffractometry showed that drug loading above the solubility limit of the drug in the polymer generated excess crystalline drug on the surface of the particles. Raman spectral mapping illustrated that drug was homogeneously distributed as a solid solution in the particles when loaded below saturation in the polymer with consequently minimal burst release. Both the manufacturing method (which influenced particle porosity and density) and drug:polymer compatibility and loading (which affected drug form and distribution) were responsible for burst release seen from our particles.

Electrospun poly (ɛ-caprolactone)/silk fibroin core-sheath nanofibers and their potential applications in tissue engineering and drug release

One of the key tenets of tissue engineering is to develop scaffold materials with favorable biodegradability, surface properties, outstanding mechanical strength and controlled drug release property. In this study, we generated core-sheath nanofibers composed of poly (ɛ-caprolactone) (PCL) and silk fibroin (SF) blends via emulsion electrospinning. Nanofibrous scaffolds were characterized by combined techniques of scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), differential scanning calorimetry (DSC), contact angle and tensile measurements. An in vitro FITC release study was conducted to evaluate sustained release potential of the core-sheath structured nanofibers. We found that the conformation of SF contained in PCL/SF composite nanofibers was transformed from random coil to β-sheet when treated with methanol, leading to improved crystallinity and tensile strength of nanofibrous scaffolds. The hydrophobicity and diameter of nanofibers decreased when we increased the content of SF in PCL/SF composite nanofibers. Furthermore, we evaluated the potential of fabricated PCL/SF composite nanofibers as scaffold in vitro. The results confirmed that fabricated PCL/SF scaffolds improved cell attachment and proliferation. Our results demonstrated the feasibility to generate core-sheath nanofibers composed of PCL and SF using a single-nozzle technique. The produced nanofibrous scaffolds with sustained drug release have potential application in tissue engineering.

Bone morphogenetic protein-2 in biodegradable gelatin and β-tricalcium phosphate sponges enhances the in vivo bone-forming capability of bone marrow mesenchymal stem cells

Bone marrow mesenchymal stem cells (MSCs) have been used for bone tissue engineering due to their osteogenic differentiation capability, but their application is controversial. To enhance their capability, we prepared biodegradable gelatin sponges incorporating β-tricalcium phosphate ceramics (GT sponge), which has been shown to possess excellent controlled drug-release properties. The GT sponge was used as a carrier for both rat MSCs and bone morphogenetic protein-2 (BMP-2) and osteogenic differentiation was assessed by subcutaneous implantation of four different kinds of implants, i.e. GT-alone, MSC-GT composites, BMP-GT composites and BMP-GT composites supplemented with MSCs (BMP-MSC-GT) in rats. Two weeks after implantation, histological sections showed new bone formation in the peripheral parts of the BMP-GT and in almost the total volume of the BMP-MSC-GT implants. After 4 weeks, histology as well as microCT analyses demonstrated extensive bone formation in BMP-MSC-GT implants. Gene expression and biochemical analyses of both alkaline phosphatase and bone-specific osteocalcin confirmed the histological findings. These results indicate that the combination of MSCs, GT and BMP synergistically enhances osteogenic capability and provides a rational basis for their clinical application in bone reconstruction.

Review of sunscreen and the emergence of non-conventional absorbers and their applications in ultraviolet protection

Protection against ultraviolet (UV) radiation is the major function of sunscreen lotions and UV-protective coatings for vehicles, homes, equipment and clothing. Sunscreen formulations have been optimized to become protective over a broader spectrum of UV radiation and maintain greater photostability. They are comprised of organic and inorganic components that act as chemical and physical UV protectors, respectively. Some of the organic components are limited by their spectrum of protection and photostability. Studies using solid lipid nanoparticles, recently explored organic molecules, inorganic components and antioxidants attempt to further optimize UV protection. In this review, we examine traditional and emerging nanoparticle components and highlight novel ideas in UV protection which may provide pathways for future studies.

Facile synthesis of an up-conversion luminescent and mesoporous Gd2O3 : Er3+@nSiO2@mSiO2nanocomposite as a drug carrier

In this paper, we report the facile synthesis of a bifunctional inorganic nanocomposite which is composed of core-shell structured mesoporous silica coated with up-conversion Gd2O3 : Er3+ particles. X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), N2 adsorption/desorption, and photoluminescence (PL) spectra were used to characterize the samples. The results indicate that the nanocomposite with general 50 nm shell thickness and 300 nm core size shows typical ordered mesoporous characteristics (2.3 nm) and has spherical morphology with smooth surface and narrow size distribution. The bifunctional system shows unique green up-conversion emission under 980 nm NIR laser excitation even after loading with drug molecules. In addition, biocompatibility tests on L929 fibroblast cells using an MTT assay reveals low cytotoxicity of the system. Drug release tests suggest that the nanocomposite has a controlled drug release property with ibuprofen (IBU) as the model drug. Interestingly, the up-conversion emission intensity of the bifunctional carrier increases with the released amount of model drug, thus allowing the release process to be monitored and tracked by the change of up-conversion luminescence intensity. This composite can potentially act as a functional drug carrier system.

Fabrication, Surface Properties and Protein Encapsulation/Release Studies of Electrospun Gelatin Nanofibers

The aim of this study was to fabricate gelatin nanofibers by electrospinning and investigate the characteristics of these nanofibers. It has been reported that composite nanofibrous mats with drug impregnated in biocompatible and biodegradable polymer nanofibers can serve as tissue-engineering scaffolds with desired and controllable drug-release properties. The composite nanofibrous mats electrospun from a solution consisting of gelatin, bovine serum albumin (BSA, a model compound to simulate proteins), poly(ethylene glycol) sorbitan monolaurate (Tween-20) and 2,2,2-trifluoroethanol (TFE) were prepared and characterized. The BSA release profile in phosphate-buffered saline (PBS, pH 7.4) was recorded and analyzed. For comparison, nanofibrous mats electrospun from the solution containing gelatin and BSA were also prepared and assessed. The morphologies of the nanofibrous mats were examined by scanning electron microscopy; the surface hydrophilicity was measured by water contact angle method; and the protein-release profiles were recorded by analyzing BSA amount after immersing the electrospun nanofibrous mats in PBS for various time periods. The results indicated that the composite nanofibrous mats electrospun from the gelatin emulsion and/or solution had controllable protein-release behavior and they could be utilized as tissue-engineering scaffolds with protein encapsulated.

Thermo-Responsive Core-Shell Composite Nanoparticles Synthesized via One-Step Pickering Emulsion Polymerization for Controlled Drug Delivery

Purpose: The focus of this work is to develop a unique drug delivery vehicle which can be taken up by cancer cells and can release the loaded drug. Methods: Core-shell composite nanoparticles have been prepared by one-step Pickering emulsion polymerization with a nonionic initiator, using silica as the sole stabilizer. More importantly, the Pickering emulsion polymerization is applied to synthesize polystyrene/poly(N-isopropylacrylamide) (PNIPAAm)-silica core-shell nanoparticles with N-isopropylacrylamide incorporated into the core as a co-monomer. Results: The composite nanoparticles are temperature sensitive and can be taken up by human prostate cancer (PC3 and PC3-PSMA) cells. An anticancer agent 17-(Allylamino)-17-demethoxygeldanamycin (17-AAG) has been loaded into the polymeric cores during formation of the nanoparticles and drug release has been successfully observed at elevated temperatures. The ability of the various nanoparticles for inducing death in human prostate cancer cells has been evaluated. Conclusion: The work has demonstrated the temperature sensitivity, controlled drug release properties of the synthesized core-shell nanoparticles, and their effectiveness for inducing death of human prostate cancer cells.

Evaluating the Controlled Release Properties of Inhaled Nanoparticles Using Isolated, Perfused, and Ventilated Lung Models

Polymeric nanoparticles meet the increasing interest for inhalation therapy and hold great promise to improve controlled drug delivery to the lung. The synthesis of tailored polymeric materials and the improvement of nanoparticle preparation techniques facilitate new perspectives for the treatment of severe pulmonary diseases. The physicochemical properties of such drug delivery systems can be investigated using conventional analytical procedures. However, the assessment of the controlled drug release properties of polymeric nanoparticles in the lung remains a considerable challenge. In this context, the isolated lung technique is a promising tool to evaluate the drug release characteristics of nanoparticles intended for pulmonary application. It allows measurements of lung-specific effects on the drug-release properties of pulmonary delivery systems.Ex vivomodels are thought to overcome the common obstacles ofin vitrotests and offer more reliable drug release and distribution data that are closer to thein vivosituation.

Preparation of 5-Fluorouracil/β-Cyclodextrin Complex Intercalated in Layered Double Hydroxide and the Controlled Drug Release Properties

Hydrophobic anticancer drug 5-fluorouracil (5-FU) has been included in the carboxymethyl modified β-cyclodextrin (CMCD), and the inclusion complex (5-FU/CMCD) was further intercalated into galleries of a zinc aluminum layered double hydroxide (ZnAl−LDH) by the ion-exchange method. Powder X-ray diffraction (XRD), Fourier transform infrared (FT-IR), and UV−vis spectroscopy indicate a successful intercalation of 5-FU/CMCD into the LDH gallery. The release behavior of 5-FU from drug/CMCD−LDH composite at different pH values was studied. It was found that 5-FU was released faster in pH 7.2 than in the acidic mediums (pH 4.8), and the released amount was higher. The introduction of CMCD into the LDH matrix could prolong the drug release time in comparison to that from LDH without CMCD, which can be attributed to the inclusion of 5-FU by the CMCD cavity. Studies on mathematical modeling of drug release show that the release of 5-FU from the drug/CMCD−LDH composite follows the Korsmeyer−Peppas equation very well ...

Polymer-conjugated albumin and fibrinogen composite hydrogels as cell scaffolds designed for affinity-based drug delivery

Serum albumin was conjugated to poly-(ethylene glycol) (PEG) and cross-linked to form mono-PEGylated albumin hydrogels. These hydrogels were used as a basis for drug carrying tissue engineering scaffold materials, based on the natural affinity of various drugs and compounds for the tethered albumin in the polymer network. The results of the drug release validation experiments showed that the release kinetics of the drugs from the mono-PEGylated albumin hydrogels were controlled by the molecular weight (MW) of PEG conjugated to the albumin protein, the drug MW and its inherent affinity for albumin. Composite hydrogels containing both mono-PEGylated albumin and PEGylated fibrinogen were used specifically for three-dimensional (3D) cell culture scaffolds, with inherent bioactivity, proteolytic biodegradability and controlled drug release properties. The specific characteristics of these complex hydrogels were governed by the ratio between the concentrations of each protein, the addition of free PEG diacrylate (PEG DA) molecules to the hydrogel matrix and the MW of the PEG conjugated to each protein. Comprehensive characterization of the drug release and degradation properties, as well as 3D cell culture experiments using these composite materials, demonstrated the effectiveness of this combined approach in creating a tissue engineering scaffold material with controlled drug release features.

Effect of vorinostat (V)-loaded PLGA nanoparticles (NP) surface modified with a PSMA ligand on prostate cancer (PC) cells.

e13629 Background: Polymeric NP can be tuned for controlled drug delivery and SM for cell-specific targeting. To overcome V concentration and time dependent reversible growth inhibition of PC cells, we designed a NP to deliver V to PC by polymeric NP that were SM with a ligand to prostate specific membrane antigen (PSMA). Methods: V was encapsulated in poly(lactic-co-glycolic acid) (PLGA) using oil in water emulsion. Pegylated (PEG) phospholipid was added to the aqueous phase for SM, electrostatic and steric stabilization, and longer circulation in vivo. For PSMA targeting, the lipid amino end was covalently modified to possess a glutamate urea with known pM Ki binding affinity to PSMA. Four NP designs were used in cytotoxicity assays : (1) V loaded PLGA NP (V-NP), (2) V loaded PLGA NP and PSMA functionalized (V-NP-PSMA), (3) no drug and PSMA functionalized NP (Bk-NP-PSMA), (4) V loaded and unmodified PEG phospholipid (V-NP-DSPE). LNCaP and PC-3 cells (104 /well) were cultured with V (0, 0.1, 0.5, 1, 5, 10, and 100 μM), or equivalent μM concentration of V-NP, V-NP-PSMA, Bk-NP-PSMA, V-NP-DSPE for up to 72hrs. Controlled release (CR) profiles were determined from incubation in PBS, cell proliferation was measured by MTT assay, and IC50 was calculated. Results: NP mean sizes were 110-130nm, and controlled release data show at least 50% release in 7 days and are ongoing. V loading of 9.5 μg V/mg PLGA was improved to over 150μg V/mg PLGA using the PEG phospholipid method. Nonlipid formulations yielded LNCaP IC50 of 8μM, whereas unencapsulated V and functionalized PEG phospholipid formulations yielded IC50 <1μM for LNCaP and PC-3. At 24hrs, V-NP-DSPE showed no cell kill in LNCaP (PSMA+) cells at concentrations of 10μM, whereas V-NP-PSMA did show suppression to less than 80% survival. By 48hrs, 10μM V-NP-PSMA induced complete cell kill compared to 40% survival in the V-NP-DSPE treated group. Conclusions: This novel SM NP design loads a high concentration of V and effective PC cell kill with non-inferior IC50 to unencapsulated drug. Ongoing studies involve characterizing the selective PSMA binding, controlled drug release properties, and optimizing these NP qualities by fraction of PEG phospholipid. No significant financial relationships to disclose.