Controlled release of drug from folate-decorated and graphene mediated drug delivery system: Synthesis,loading efficiency,and drug release response

A novel folate-decorated and graphene mediated drug delivery system was prepared that involves uniquely combining graphene oxide (GO) with anticancer drug for controlled drug release. The nanocarrier system was synthesized by attaching doxorubicin (DOX) to graphene oxide via strong π–π stacking interaction, followed by encapsulation of graphene oxide with folic acid conjugated chitosan. The π–π stacking interaction, simplified as a non-covalent type of functionalization, enables high drug loading and subsequent controlled release of the drug. The encapsulated graphene oxide enhanced the stability of the nanocarrier system in aqueous medium because of the hydrophilicity and cationic nature of chitosan. The loading and release of DOX indicated strong pH dependence and imply hydrogen-bonding interaction between graphene oxide and DOX. The proposed strategy is advantageous in terms of targeted drug delivery and has high potential to address the current challenges in drug delivery. Thus, the prepared nanohybrid system offers a novel formulation that combines the unique properties of a biodegradable material, chitosan, and graphene oxide for biomedical applications.     

In vitro evaluation of the release of albuterol sulfate from polymer gels: effect of fatty acids on drug transport across biological membranes

In this investigation, the diffusion of the beta 2 agonist albuterol sulfate (ABS) across several membranes (cellulose, hairless mouse skin, human cadaver skin) from polymer gels was studied, and the effects of several fatty acids on drug permeation through skin were evaluated. The results were then used to predict whether transdermal delivery would be appropriate for ABS. All in vitro release studies were carried out at 37 degrees C using modified Franz diffusion cells. In preliminary studies, ABS release through cellulose membranes was studied from two polymeric gels, Klucel (hydroxypropylcellulose) and Methocel (hydroxypropylmethylcellulose). Three polymer concentrations were used for each gel (0.5%, 1.0%, and 1.5%). From these experiments, Klucel 0.5% was selected as the optimal formulation to study ABS diffusion across hairless mouse skin. Experiments were conducted to evaluate the effects of capric acid, lauric acid, and myristic acid as penetration enhancers. The results suggested that lauric acid preferentially enhanced ABS diffusion compared to the other fatty acids studied, and follow-up studies were done to evaluate the release through human cadaver skin from a donor containing 2% ABS and lauric acid in 0.5% Klucel. These experiments showed that a 2:1 (lauric acid:ABS) molar ratio gave the best ABS release rates. The release rate across human cadaver skin declined slowly over 24 hr, and an average flux over 24 hr of approximately 0.09 mg/hr cm2 was measured. Using this value as a steady-state flux, extrapolations predicted that transdermal delivery can be used to maintain therapeutic ABS plasma levels (6-14 ng/mL) for extended periods. The results of this research suggest that ABS is a good candidate for transdermal drug delivery.     

Size effect of PLGA spheres on drug loading efficiency and release profiles

Drug delivery systems (DDS) based on poly (lactide-co-glycolide) (PLGA) microspheres and nanospheres have been separately studied in previous works as a means of delivering bioactive compounds over an extended period of time. In the present study, two DDS having different sizes of the PLGA spheres were compared in morphology, drug (dexamethasone) loading efficiency and drug release kinetics in order to investigate their feasibility with regard to production of medical combination devices for orthopedic applications. The loaded PLGA spheres have been produced by the oil-in-water emulsion/solvent evaporation method following two different schemes. Their morphology was assessed by scanning electron microscopy and the drug release was monitored in phosphate buffer saline solution at 37°C for 550 h using high performance liquid chromatography. The synthesis schemes used produced spheres with two different and reproducible size ranges (20 ± 10 and 1.0 ± 0.4 μm) having a smooth outer surface and regular shape. The drug loading efficiency of the 1.0 μm spheres was found to be 11% as compared to just 1% for the 20 μm spheres. Over the 550 h release period, the larger spheres (diameter 20 ± 10 μm) released 90% of the encapsulated dexamethasone in an approximately linear fashion whilst the relatively small spheres (diameter 1.0 ± 0.4 μm) released only 30% of the initially loaded dexamethasone, from which 20% within the first 25 h. The changes observed were mainly attributed to the difference in surface area between the two types of spheres as the surface texture of both systems was visibly similar. As the surface area per unit volume increases in the synthesis mixture, as is the case for the 1.0 μm spheres formulation, the amount of polymer-water interfaces increases allowing more dexamethasone to be encapsulated by the emerging polymer spheres. Similarly, during the release phase, as the surface area per unit volume increases, the rate of inclusion of water into the polymer increases, permitting faster diffusion of dexamethasone.     

In vitro comparative study of drug loading and delivery properties of bioresorbable microspheres and LC bead

Drug loadable bioresorbable microspheres (BRMS) are specially designed for the treatment of hypervascular tumors through arterial embolization. These microspheres consist of carboxymethyl chitosan crosslinked with carboxymethyl cellulose, and are available at different size ranges varying from 50 to 900?µm in diameter. Similar to commercially available non-resorbable drug eluting microspheres, LC Bead^® microspheres (LCB), BRMS were capable of loading more than 99?% of doxorubicin, an anticancer drug, from the solution within 2?h with highly similar kinetics (difference factor f ₁?=?0.36; similarity factor f ₂?=?97.99). Doxorubicin loaded BRMS exhibited the highest elution rate in the 30?% ethanol aqueous solution saturated with potassium chloride, and the elution time depended on the ratio between the amount of loaded BRMS and the volume of elution media. After injection through microcatheters, BRMS have a higher recovery rate of the microsphere weight than LCB (90.96 vs. 79.63?%, P?=?0.026). Although loaded BRMS eluted more drug into the injection medium than loaded LCB (8.63 vs. 3.80?%, P?=?0.0015), there was no significant difference in the drug delivery rate between BRMS and LCB (83.88 vs. 86.65?%, P?=?0.504). This study compares the loading capability as well as the drug delivery rate of BRMS and a commercial product under a condition simulating a transcatheter arterial chemoembolization procedure and demonstrates the potential of drug loaded BRMS for the treatment of hypervascular tumors such as hepatocellular carcinoma.     

SN-38 loading capacity of hydrophobic polymer blend nanoparticles: formulation,optimization and efficacy evaluation

One of the most important problems in nanoencapsulation of extremely hydrophobic drugs is poor drug loading due to rapid drug crystallization outside the polymer core. The effort to use nanoprecipitation, as a simple one-step procedure with good reproducibility and FDA approved polymers like Poly(lactic-co-glycolic acid) (PLGA) and Polycaprolactone (PCL), will only potentiate this issue. Considering that drug loading is one of the key defining characteristics, in this study we attempted to examine whether the nanoparticle (NP) core composed of two hydrophobic polymers will provide increased drug loading for 7-Ethyl-10-hydroxy-camptothecin (SN-38), relative to NPs prepared using individual polymers. D-optimal design was applied to optimize PLGA/PCL ratio in the polymer blend and the mode of addition of the amphiphilic copolymer Lutrol^®F127 in order to maximize SN-38 loading and obtain NPs with acceptable size for passive tumor targeting. Drug/polymer and polymer/polymer interaction analysis pointed to high degree of compatibility and miscibility among both hydrophobic polymers, providing core configuration with higher drug loading capacity. Toxicity studies outlined the biocompatibility of the blank NPs. Increased in vitro efficacy of drug-loaded NPs compared to the free drug was confirmed by growth inhibition studies using SW-480 cell line. Additionally, the optimized NP formulation showed very promising blood circulation profile with elimination half-time of 7.4?h.     

The influence of polymer blend composition on the degradation of polymer/hydroxyapatite biomaterials

The in vitro degradation of biodegradable polymer/ceramic composites was assessed in two different environments under both static and pseudodynamic conditions. The blends, consisting of polycaprolactone, poly(lactic-co-glycolic acid), and hydroxyapatite, have potential use in bone tissue engineering applications, thus it is essential to establish a standardized method of characterizing the degradation of new biomaterials. In this study, the variation in polymer blend ratio was examined to observe a change in degradation rate. The porous blends were degraded in water and serum-containing media. A previous study examined in vitro degradation in serum-free buffer. Molecular weight loss, gravimetric weight loss, pH changes and morphological changes were evaluated. The changes in porosity were observed with scanning electron microscopy and quantitatively assessed using image analysis. There was a significant difference in molecular weight loss and gravimetric weight loss between the blends after 10 weeks in vitro. Blends containing the greatest amount of poly(lactic-co-glycolic acid) degraded most rapidly. © 2001 Kluwer Academic Publishers     

In vitro iontophoretic release of lithium chloride and lidocaine hydrochloride from polymer electrolytes

Ionically conducting polymers, frequently known as polymer electrolytes, are potential candidates as hosts for drugs to be delivered iontophoretically. The iontophoretic delivery of lithium or lidocaine from polymer electrolyte films through a cellophane membrane was examined using different delivery current regimes. Thin, mechanically strong, polymer electrolyte films were fabricated from poly(ethylene oxide) (PEO) with lithium chloride or lidocaine hydrochloride. Experiments showed that iontophoretic transport of both lithium chloride and lidocaine hydrochloride might be achieved from these PEO-based films. Cation transport number determinations give values for PEO-based films of about 0.4 for lithium chloride systems and 0.12 for lidocaine hydrochloride systems. The mechanism of transport from these PEO-based polymer electrolyte films allows the delivery of ionic salts such as lithium chloride and lidocaine hydrochloride to be controlled solely by current, thus providing a system that can deliver precise amounts of drug.     

In vitro release of ketoprofen from hydrophilic matrix tablets containing cellulose polymer mixtures

The effect of cellulose ether polymer mixtures, containing both hydroxypropylcellulose (HPC) and hydroxypropylmethylcellulose (HPMC K15M or K100M), on ketoprofen (KTP) release from matrix tablets was investigated. In order to evaluate the compatibility between the matrix components, Raman spectroscopy, scanning electron microscopy (SEM), and X-ray powder diffraction (XRPD) experiments were performed. The results evidence the absence of significant intermolecular interactions that could eventually lead to an incompatibility between the drug and the different excipients. Formulations containing mixtures of polymers with both low and high viscosity grades were prepared by a direct compression method, by varying the polymer/polymer (w/w) ratio while keeping the drug amount incorporated in the solid dispersion constant (200?mg). The hardness values of different matrices were found within the range 113.8 to 154.9 N. HPLC analysis showed a drug content recovery between 99.3 and 102.1%, indicating that no KTP degradation occurred during the preparation process. All formulations attained a high hydration degree after the first hour, which is essential to allow the gel layer formation prior to tablet dissolution. Independent-model dissolution parameters such as t_10% and t_50% dissolution times, dissolution efficiency (DE), mean dissolution time (MDT), and area under curve (AUC) were calculated for all formulations. Zero-order, first-order, Higuchi, and Korsmeyer–Peppas kinetic models were employed to interpret the dissolution profiles: a predominantly Fickian diffusion release mechanism was obtained – with Korsmeyer–Peppas exponent values ranging from 0.216 to 0.555. The incorporation of HPC was thus found to play an essential role as a release modifier from HPMC containing tablets.     

Hydrogel containing dexamethasone-loaded nanocapsules for cutaneous administration: preparation,characterization, and in vitro drug release study

Context: Our group previously reported the development of dexamethasone-loaded polymeric nanocapsules as an alternative for topical dermatological treatments. Objective: Our study aimed to prepare and characterize a hydrogel containing this system to improve the effectiveness of the glucocorticoid for cutaneous disorders. Methods: For the antiproliferative activity assay, a dexamethasone solution and D-NC were tested on Allium cepa root meristem model. D-NC were prepared by the interfacial deposition of preformed polymer. Hydrogels were prepared using Carbopol Ultrez® 10 NF, as polymer, and characterized according to the following characteristics: pH, drug content, spreadability, viscosity, and in vitro drug release. Results and Discussion: Nanocapsules showed mean particle size and zeta potential of 201 ± 6 and ?5.73 ± 0.42 nm, respectively. They demonstrated a lower mitotic index (4.62%) compared to free dexamethasone (8.60%). Semisolid formulations presented acidic pH values and adequate drug content (between 5.4% and 6.1% and 100% and 105%, respectively). The presence of nanocapsules in hydrogels led to a decrease in their spreadability factor. Intact nanoparticles were demonstrated by TEM as well as by dynamic light scattering (mean particle size < 300 nm). In vitro studies showed a controlled dexamethasone release from hydrogels containing the drug associated to the nanocapsules following the Higuchi's squared root model (k = 20.21 ± 2.96 mg/cm²/h^1/2) compared to the hydrogels containing the free drug (k = 26.65 ± 2.09 mg/cm²/h^1/2). Conclusion: Taking all these results together, the hydrogel containing D-NC represent a promising approach to treat antiproliferative-related dermatological disorders.     

In vitro release profile of anti-ulcer drug rabeprazole from biocompatible psyllium-PVA hydrogels

The present article discusses the synthesis, characterization and haemocompatibility behaviour of the psyllium-PVA hydrogels prepared by chemical method in the presence of N,N′-methylenebisacrylamide. These hydrogels have been characterized by Fourier Transform infrared spectroscopy, thermo gravimetric analysis, swelling and drug release studies. The release of model drug rabeprazole sodium from the drug loaded hydrogels occurred through non-Fickian diffusion mechanism. Psyllium itself acts as anti-ulcer agent and release of rabeprazole from the drug loaded hydrogels may enhance the curing potential of the drug delivery device. The haemocompatibility was evaluated by studying the blood interactions with hydrogels with reference to thrombogenicity and haemolytic potential. Thrombogenicity results indicate that hydrogels are non-thrombogenic as the weight of clot formed and thrombus percentage for hydrogels was less than the positive control. The haemolytic index has been observed <5%. These observations indicate that these hydrogels are haemo-compatible and hence could be used for oral administration of antiulcer drugs.     

In vitro release study of transdermal delivery systems of progesterone

A potential transdermal application of progesterone was investigated. In vitro diffusion studies of the drug were performed. Investigations were carried out in order to examine if the addition of urea, pantothenol, or laurocapram can enhance the release rates from Eud (Eudragit NE 30 D) matrices. Pantothenol and urea increased the release 1.4- to 1.6-fold. The transdermal therapeutic system (TTS) containing 10% laurocapram delivered the highest release rates with a 2.8-fold enhancement.     

Gellan gum microspheres crosslinked with trivalent ion: effect of polymer and crosslinker concentrations on drug release and mucoadhesive properties

Gellan gum microspheres were obtained by ionotropic gelation technique, using the trivalent ion Al³⁺. The percentage of entrapment efficiency ranged from 48.76 to 87.52% and 2² randomized full factorial design demonstrated that both the increase of polymer concentration and the decrease of crosslinker concentration presented a positive effect in the amount of encapsulated drug. Microspheres size and circularity ranged from 700.17 to 938.32?μm and from 0.641 to 0.796?μm, respectively. The increase of polymer concentration (1–2%) and crosslinker concentration (3–5%) led to the enlargement of particle size and circularity. However, the association of increased crosslinker concentration and reduced polymer content made the particles more irregular. In vitro and ex vivo tests evidenced the high mucoadhesiveness of microspheres. The high liquid uptake ability of the microspheres was demonstrated and the pH variation did not affect this parameter. Drug release was pH dependent, with low release rates in acid pH (42.40% and 44.93%) and a burst effect in phosphate buffer pH (7.4). The Weibull model had the best correlation with the drug release data, demonstrating that the release process was driven by a complex mechanism involving the erosion and swelling of the matrix or by non-Fickian diffusion.     

Durability of polymer matrix composites: Viscoelastic effect on static and fatigue loading

The structural applications of polymer matrix composites (PMC) demand lifetimes of 15, 25 and 50 years. However, the mechanical properties of these composites have a time dependent nature, i.e. strength and stiffness are time-dependent due to the hereditary nature (viscoelasticity) of polymers. In this context lifetime models for viscoelastic materials, i.e. energy-based criteria and fracture mechanics extended to viscoelastic media, are revised. These models are applied to predict the lifetime of composite materials under special cases of constant load (creep rupture) and constant stress rate to failure. It is verified that these lifetime theories predict similar relationship between creep failure and constant stress rate failure strength. Alternative approaches based on Strength Evolution Integral [Reifsnider KL, Stinchcomb WW. A critical element model of the residual strength and life of fatigue–loaded composite coupons. In: Hahn HT, editor. Composite materials: fatigue and fracture (ASTM STP 907). Philadelphia (PA): American Society for Testing and Materials; 1986. p. 298–313; Reifsnider KK, Case SC, Duthoi J. The mechanics of composite strength evolution. Compos Sci Technol 2000; 60:2539–46; Reifsnider KK, Case SC. Damage tolerance and durability in material systems. Wiley-Interscience; 2002] and on Linear Damage Accumulation (LCD) law confirm these results. In addition the LCD law was found to be generally unsatisfactory except for the special case of constant stress rate to failure. Accordingly this result validates the accelerated methodology proposed by [Miyano Y, McMurray M, Enyama J, Nakada M. Loading rate and temperature dependence on flexural fatigue behavior of a satin woven CFRP laminate. J Compos Mater 1994;28(13):1250–60; Miyano Y, Nakada M, McMurray MK, Muki R. Prediction of flexural fatigue strength of CRFP composites under arbitrary frequency, stress ratio and temperature. J Compos Mater 1997;31(6):619–38; Miyano Y, Nakada M, Kudoh H, Muki R. Prediction of tensile fatigue life for unidirectional CFRP. J Compos Mater 2000;34(7):538–50; Miyano Y, Nakada M, Sekine N. Accelerated testing for long-term durability of GFRP laminates for marine use. Compos: Part B 2004;35:497–502; Miyano Y, Nakada M, Sekine N. Accelerated testing for long-term durability of FRP laminates for marine use. J Compos Mater 2005;39(1):5–20], which is based on LCD law, to characterize long-term creep failure of polymer composites based on the constant stress rate failure strength curves.Finally a new formulation is proposed, based on Strength Evolution Integral, to predict of fatigue failure load for an arbitrary load ratio.     

Beclomethasone-loaded lipidic nanocarriers for pulmonary drug delivery: preparation, characterization and in vitro drug release

The purpose of this research paper was the development of lipid nanoparticles (LN) formulation suitable for beclomethasone dipropionate (BDP) administration via the pulmonary route. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were prepared by high-shear homogenization method; the effects of process and formulation parameters on nanoparticles characteristics were investigated. LN were characterized in terms of morphology, size, encapsulation efficiency, in vitro drug release and aerosol aerodynamic properties. Nano-sized BDP-loaded LN with high entrapment efficiency values reaching 99% were successfully obtained. Application of in vitro drug release data to the Higuchi kinetic equation indicated a diffusion-controlled release from the lipidic matrix. Aerosolisation and subsequent cascade impaction measurements proved that SLN and NLC were efficiently nebulized yielding aerosols of a suitable particle size for BDP deep lung delivery. Results demonstrate that LN are promising nebulized carriers for BDP opening the way for lipophilic drug-targeting strategies by nebulization.     

Local drug delivery system for the treatment of osteomyelitis: In vitro evaluation

Local antimicrobial delivery is a potential area of research conceptualized to provide alternative and better methods of treatment for cases, as osteomyelitis where avascular zones prevent the delivery of drugs from conventional routes of administration. Drug-loaded polymers and calcium phosphates as hydroxyapatites have been tried earlier. Bioactive glasses are bone-filling materials used for space management in orthopedic and dental surgery. A new bioactive glass (SSS2) was synthesized and fabricated into porous scaffold with a view to provide prolonged local delivery of gatifloxacin and fluconazole as suitable for the treatment of osteomyelitis. The new SSS2 was characterized by Fourier transform infrared (FTIR) and X-ray diffraction (XRD) analyses. In addition, the bioactivity of the SSS2 glass and resulting scaffold was examined by in vitro acellular method and ascertained by FTIR and XRD. The pore size distribution was analysed by mercury intrusion porosimetry and the release of drugs from scaffolds were studied in vitro. The glass and the resulting scaffolds were bioactive indicating that they can bond with bone in vivo. The scaffolds were porous with pores predominantly in the range of 10–60 µm, released the drugs effectively for 6 weeks and deemed suitable for local delivery of drugs to treat osteomyelitis.     

Local drug delivery system for the treatment of osteomyelitis: In vitro evaluation

Local antimicrobial delivery is a potential area of research conceptualized to provide alternative and better methods of treatment for cases, as osteomyelitis where avascular zones prevent the delivery of drugs from conventional routes of administration. Drug-loaded polymers and calcium phosphates as hydroxyapatites have been tried earlier. Bioactive glasses are bone-filling materials used for space management in orthopedic and dental surgery. A new bioactive glass (SSS2) was synthesized and fabricated into porous scaffold with a view to provide prolonged local delivery of gatifloxacin and fluconazole as suitable for the treatment of osteomyelitis. The new SSS2 was characterized by Fourier transform infrared (FTIR) and X-ray diffraction (XRD) analyses. In addition, the bioactivity of the SSS2 glass and resulting scaffold was examined by in vitro acellular method and ascertained by FTIR and XRD. The pore size distribution was analysed by mercury intrusion porosimetry and the release of drugs from scaffolds were studied in vitro. The glass and the resulting scaffolds were bioactive indicating that they can bond with bone in vivo. The scaffolds were porous with pores predominantly in the range of 10-60 μm, released the drugs effectively for 6 weeks and deemed suitable for local delivery of drugs to treat osteomyelitis.     

In vitro study of vancomycin release and osteoblast-like cell growth on structured calcium phosphate-collagen

A drug delivery vehicle consisting of spherical calcium phosphate-collagen particles covered by flower-like (SFCaPCol) blossoms composed of nanorod building blocks and their cellular response is studied. The spherical structure was achieved by a combination of sonication and freeze-drying. The SFCaPCol blossoms have a high surface area of approximately 280 m²g^? 1. The blossom-like formation having a high surface area allows a drug loading efficiency of 77.82%. The release profile for one drug, vancomycin (VCM), shows long term sustained release in simulated body fluid (SBF), in a phosphate buffer saline (PBS, pH 7.4) solution and in culture media over 2 weeks with a cumulative release ~ 53%, 75% and 50%, respectively, over the first 7 days. The biocompatibility of the VCM-loaded SFCaPCol scaffold was determined by in vitro cell adhesion and proliferation tests of rat osteoblast-like UMR-106 cells. MTT tests indicated that UMR-106 cells were viable after exposure to the VCM loaded SFCaPCol, meaning that the scaffold (the flower-like blossoms) did not impair the cell's viability. The density of cells on the substrate was seen to increase with increasing cultured time.     

Reactive calcium-phosphate-containing poly(ester-co-ether) methacrylate bone adhesives: setting, degradation and drug release considerations

This study has investigated novel bone adhesives consisting of fluid photo-polymerizable poly(lactide-co-propylene glycol-co-lactide)dimethacrylate (PGLA-DMA) mixed with systematically varying fillers of β-tricalcium phosphate (β-TCP) and monocalcium phosphate monohydrate (MCPM), for the delivery of an antibacterial drug chlorhexidine (CHX). All formulations were found to polymerize fully within 200 s after exposure to blue light. In addition, water sorption by the polymerized materials catalyzed varying filler conversion to dicalcium phosphate (DCP) (i.e. brushite and monetite). With greater DCP levels, faster degradation was observed. Moreover, increase in total filler content enhanced CHX release, associated with higher antibacterial activity. These findings thus suggest that such rapid-setting and degradable adhesives with controllable drug delivery property could have potential clinical value as bone adhesives with antibacterial activity.     

In vitro release studies on matrix type transdermal drug delivery systems of naltrexone and its acetyl prodrug

Matrix type acrylic adhesive transdermal patches of naltrexone (NTX) and its 3-O-acetyl ester prodrug were prepared and evaluated for drug content, thickness, and in vitro release characteristics. Among the four DURO-TAK adhesive polymers (87-2516, 87-2054, 87-2501, and 87-2582) tested, 87-2516 proved to be the most suitable and compatible polymer for the transdermal delivery of NTX from NTX and prodrug patches. A linear relationship was observed for release flux (F) and cumulative amount (Mt) values versus 1%, 2%, and 3% drug loading at equimolar levels. The release of NTX from the patches showed a good correlation (R2>0.99) for Mt vs. square root t profiles, indicating that a Higuchian matrix diffusion mechanism of drug release from the transdermal adhesive patches was obtained. Overall, the amounts of NTX released from the prodrug patches were significantly higher than from the NTX patches, at all three drug loading levels.     

In vitro evaluation and finite element simulation of drug release from polydiacetylene-polyethylene glycol stearate nanovesicles

Vesicles comprised of 10,12-pentacosadiynoic acid (PCDA) were modified, using polyethylene glycol 40 stearate (PEG40S), and crosslinked by ultraviolet (UV) irradiation to create polymerized nanovesicles for sustained drug release. Paclitaxel, a water-insoluble compound widely used in cancer chemotherapy, was used as a model drug to examine the physicochemical stability and release profiles of PCDA/PEG40S nanovesicles. TEM analysis revealed the formation of paclitaxel-encapsulated PCDA/PEG40S nanovesicles of 40 to 200 nm in size. Upon the addition of ethanol, instantaneous releases of paclitaxel in the amount of 28 microg/mL from polymerized PCDA/PEG40S nanovesicles and 108 microg/ml from unpolymerized ones were observed. This suggested the non-complete drug release from polymerized PCDA/PEG40S nanovesicles due to their enhanced physicochemical stability by ultraviolet irradiation-induced polymerization, if compared to unpolymerized ones. An in vitro study demonstrated that an accumulative release of 24.1 +/- 3.1% and 8.1 +/- 1.7% of paclitaxel was obtained within 24 hrs from nanovesicles comprised of PCDA/PEG40S at a 9:1 and 7:3 molar ratio, respectively. A finite element model that considered the diffusion-driven releases and the reversible drug-vesicle interaction captured the sustained release of paclitaxel from polymerized PCDA/PEG40S nanovesicles. PCDA/PEG40S nanovesicles capable of sustained release and with enhanced physicochemical stability thus possess great potential for applications in drug release.