An overview of the emerging warm mix asphalt technology

The asphalt industry is constantly attempting to reduce its emissions as concerns are growing on global warming. This is done by decreasing the mixing and compaction temperatures of asphalt mixtures without affecting the properties of the mix which is possible through numerous available technologies in the industry. The production of asphalt mix is done by warm mix asphalt (WMA) technology at considerably lower temperatures (120°C or lower). Less energy consumption, lower mixing and compaction temperatures, early site opening, reduced ageing, fewer emissions, cool weather paving, better workability and, finally, an extended paving window could be mentioned as some of the benefits obtained by using the WMA. This paper presents the WMA techniques and technologies such as foaming techniques, wax and chemical additives techniques. Additionally, the performance of WMA popular technologies such as Sasobit^®, WAM^®-Foam, Evotherm^®, Low energy asphalt, Rediset^® WMX and REVIX? are fully described.     

Field performance of top-down fatigue cracking for warm mix asphalt pavements

As a result of repeated rehabilitation efforts over the past few decades, often asphalt pavements have become deep-strength pavements. Consequently, top-down cracking has become a primary distress type. In particular, the top-down cracking performance of warm mix asphalt (WMA) pavements, i.e. how does it compare with similar hot mix asphalt (HMA) pavements is largely unclear mainly due to the lack of field performance data. This paper presents an effort of monitoring the top-down cracking performance of 28 pavement projects including WMA pavements and their corresponding HMA control pavements with service lives ranging between 4 and 10 years. These pavements cover different climate zones, WMA technologies, service years, pavement structures and traffic volume levels. Two rounds of distress surveys were conducted at a two-year interval, and the material (asphalt binder and mixture) properties of the pavements were determined using field cores. The top-down cracking performance of the HMA and WMA pavements was compared based on the first and second round distress surveys. It was found that the HMA and WMA pavement in general exhibited comparable performance. The significant determinants (material properties) for top-down cracking were determined, which were vertical failure deformation of mixes measured at 20 °C from indirect tension test.     

The effect of aggregate gradation on creep and moisture susceptibility performance of warm mix asphalt

It is clear that the purpose of mixture design is to select optimum asphalt content for a desired aggregate structure to meet the prescribed criteria. Aggregate makes up high proportion of volume and mass of mixtures; hence, it is considered as an important constituent of asphalt concrete. This study postulates that the gradation is an important characteristic of the aggregate in adoption of the optimum mixture. One aggregate source, three gradations and different percentages of Sasobit^® was used to manufacture hot mix asphalt and warm mix asphalt. The test results indicated that the aggregate gradation affects the rutting resistance and especially the moisture susceptibility of the introduced mixtures, differently. Rutting resistance was evaluated using the flow number parameter, and in order to determine the moisture sensitivity mechanism, a mechanical and visual inspection tests were carried out. At the end, it is concluded that the optimum aggregate gradation for these two types of mixtures is different.     

Performance evaluation of WMA plant and field trial mixes

Warm mix asphalt (WMA) technology is still in its infancy, with significant scope for further exploration of the benefits of incorporation of higher percentages of recycled asphalt RA as well as modified binders for performance enhancement. The objective of this study was to evaluate three different WMA technologies, namely chemical and organic additives as well as foamed technology, within different mix compositions. The variables in mix composition included 10–20 % RA in surfacing mixes and 20–40 % RA in base layer mixes. The binder variables included two base binders, control mixes (no modifier) and ethylene vinyl acetate (EVA) or styrene butadiene styrene (SBS) with or without WMA technologies. A partial factorial experimental design based on the above variables was developed. Full-scale plant mixes and field (construction) mixes were produced and beams were prepared from compacted slabs and tested under 4 point loading to provide master curves and fatigue relations. Comparative results show inconsistent trends between different technologies. control mixes (HMA) can provide both higher and lower flexural stiffness than their WMA counterparts. EVA or SBS modification can provide either superior or inferior mixes to their WMA counterparts depending on the WMA technology. Generally the fatigue results of both the HMA surfacing and base layer mixes at both RA contents are superior to their equivalent WMA counterparts. The implications of these differences are explored in the publication.     

Fatigue life and endurance limit prediction of asphalt mixtures using energy-based failure criterion

Fatigue cracking is one of the major types of distress in asphalt mixtures and is caused by the accumulation of damage in pavement sections under repeated load applications. The fatigue endurance limit (EL) concept assumes a specific strain level, below which the damage in hot mix asphalt (HMA) is not cumulative. In other words, if the asphalt layer depth is controlled in a way that keeps the critical HMA flexural strain level below the EL, the fatigue life of the mixture can be extended significantly. This paper uses two common failure criteria, the traditional beam fatigue criterion and the simplified viscoelastic continuum damage model energy-based failure criterion (the so-called G^R method), to evaluate the effect of different parameters, such as reclaimed asphalt pavement (RAP) content, binder content, binder modification and warm mix asphalt (WMA) additives, on the EL value. In addition, both failure criteria are employed to investigate the impacts of these parameters in terms of the fatigue life of the study mixtures. According to the findings, unlike an increase in RAP content, which has a negative effect on the mixtures’ fatigue resistance, a higher binder content and/or binder modification can significantly increase the EL value and extend the fatigue life as was proved before by other researchers, whereas WMA additives do not significantly affect the mixtures’ fatigue behaviour. A comparison of the model simulation results with the field observations indicates that the G^R method predicts the field performance more accurately than the traditional method.     

Nanostructured lipid carriers loaded with simvastatin: effect of PEG/glycerides on characterization,stability, cellular uptake efficiency and in vitro cytotoxicity

Objective: The aim of this study is to evaluate the use of PEG/glycerides of different HLB; oleoyl macrogol-6-glycerides (Labrafil^® M 1944 CS) and caprylocaproylmacrogol-8-glycerides (Labrasol^®), compared to Labrafac lipophile^® as PEG-free glyceride in the preparation of nanostructured lipid carriers (NLCs). PEG/glycerides are suggested to perform a dual function; as the oily component, and as the PEG-containing substrate required for producing the PEGylated carriers without physical or chemical synthesis.

Methods: Lipid nanocarriers were loaded with simvastatin (SV) as a promising anticancer drug. An optimization study of NLC fabrication variables was first conducted. The effect of lyophilization was investigated using cryoprotectants of various types and concentrations. The prepared NLCs were characterized in terms of particle size (PS), size distribution (PDI), zeta potential (ZP), drug entrapment, in vitro drug release, morphology and drug–excipient interactions. The influence of glycerides?±?PEG on the cytotoxicity of SV was evaluated on MCF-7 breast cancer cells, in addition to the cellular uptake of fluorescent blank NLCs.

Results: The alteration between different oil types had a significant impact on PS, ZP and drug release. Both sucrose and trehalose showed the lowest increase in PS and PDI of the reconstituted lyophilized NLCs. The in vitro cytotoxicity and cellular uptake studies indicated that SV showed the highest antitumor effect on MCF-7 cancer cells when loaded into Labrasol^® NLCs demonstrating a high cellular uptake as well.

Conclusion: The study confirms the applicability of PEG/glycerides in the development of NLCs. Encapsulating SV in Labrasol^®-containing NLC could enhance the antitumor effect of the drug.     

Innovation of novel ‘Tab in Tab’ system for release modulation of milnacipran HCl: optimization,formulation and in vitro investigations

The study was aimed toward development of modified release oral drug delivery system for highly water soluble drug, Milnacipran HCl (MH). Novel Tablet in Tablet system (TITs) comprising immediate and extended release dose of MH in different parts was fabricated. The outer shell was composed of admixture of MH, lactose and novel herbal disintegrant obtained from seeds of Lepidium sativum. In the inner core, MH was matrixed with blend of hydrophilic (Benecel^®) and hydrophobic (Compritol^®) polymers. 3² full factorial design and an artificial neuron network (ANN) were employed for correlating effect of independent variables on dependent variables. The TITs were characterized for pharmacopoeial specifications, in vitro drug release, SEM, drug release kinetics and FTIR study. The release pattern of MH from batch A10 containing 25.17% w/w Benecel^® and 8.21% w/w of Compritol^® exhibited drug release pattern close proximal to the ideal theoretical profile (t_50% = 5.92?h, t_75% = 11.9?h, t_90% = 18.11 h). The phenomenon of drug release was further explained by concept of percolation and the role of Benecel^® and Compritol^® in drug release retardation was studied. The normalized error obtained from ANN was less, compared with the multiple regression analysis, and exhibits the higher accuracy in prediction. The results of short-term stability study revealed stable chataracteristics of TITs. SEM study of TITs at different dissolution time points confirmed both diffusion and erosion mechanisms to be operative during drug release from the batch A10. Novel TITs can be a succesful once a day delivery system for highly water soluble drugs.     

Immediate release of ibuprofen from Fujicalin®-based fast-dissolving self-emulsifying tablets

Background: Drug release from a solid form of self-emulsifying drug delivery system (SEDDS) has greatly been limited due to strong adsorption and physical interaction with carriers. To facilitate drug release process in the stomach, an acid-soluble powderizing carrier, Fujicalin^® was evaluated together with different disintegrants and hydrophilic lubricants. Method: Immediate-release self-emulsifying tablets (IR-SETs) of ibuprofen (IBU) was prepared with solidified SEDDS of IBU, various disintegrants, and lubricants, and drug release was evaluated to develop IR-SET that can release IBU with a similar IBU release rate to that obtained with liquid SEDDS. Results: The liquid SEDDS consisted of Capryol 90, Cremophor EL, Labrasol, and IBU at a ratio of 3:4:3:3, and was solidified with various adsorbents. The powderized SEDDS was tabletted by a direct compression. Fujicalin^®-based SEDDS tablets demonstrated remarkably higher dissolution rate of IBU compared with Neusilin^® and Neosyl^®-based SEDDS tablets. The IR-SET formula of IBU prepared with Fujicalin^® as an adsorbent, Polyplasdone^® as a disintegrant, and sodium bicarbonate as a co-disintegrant showed over 90% of initially loaded dose of IBU released within 5?min in a stimulated gastric juice (pH 1.2), exhibiting almost equivalent rate of IBU release to that shown by liquid SEDDS. The particle size analysis revealed no significant differences in droplet sizes of the microemulsions formed from liquid (116?nm) and IR-SET (110?nm). Conclusion: The novel IR-SET can be promising as a fast-releasing SEDDS tablet of IBU for fast onset of action.     

Eudragit® RS PO/RL PO as rate-controlling matrix-formers via roller compaction: Influence of formulation and process variables on functional attributes of granules and tablets

The influence of plasticizer level, roll pressure and sintering temperature was investigated on the granule properties, tablet breaking force and theophylline release from tablets. Nine formulations using theophylline as a model drug, Eudragit^® RL PO, Eudragit^® RS PO, or both as a matrix former and triethyl citrate (TEC) as a plasticizer were prepared. The formulations were roller compacted and the granules obtained were evaluated for particle size distribution and flowability. These granules were compacted into tablets at a compression force of 7?kN. The tablets were thermally treated at different temperatures (50 and 75°C) for 5?h and were evaluated for breaking force and dissolution. Increase in roll pressure and TEC levels resulted in a progressive increase in the mean particle size of the granules. The flowability of the granules also improved with increasing roll pressures and TEC levels. Tablet breaking force increased with an increase in TEC levels and sintering temperatures. But these effects were significant only at the highest level of plasticizer and sintering temperature respectively. For the tablets containing Eudragit^® RS PO, theophylline release decreased proportionately with increase in TEC levels and sintering temperatures. Tablets containing either Eudragit^® RL PO or a mixture of RS PO and RL PO failed to impart an extended-release property to the tablets at the studied variables i.e. roll pressure, TEC levels and sintering temperature. It was clearly demonstrated that with suitable optimization of these parameters, the release-rate of a water soluble drug from the matrix tablets prepared via roller compaction can be finely controlled.     

Development and evaluation of a novel drug delivery: Soluplus®/TPGS mixed micelles loaded with piperine in vitro and in vivo

Background: Although piperine can inhibit cells of tumors, the poor water solubility restricted its clinical application. This paper aimed to develop mixed micelles based on Soluplus^® and D-α-tocopherol polyethylene glycol succinate (TPGS) to improve the aqueous solubility and anti-cancer effect.

Methods: Piperine-loaded mixed micelles were prepared using a thin-film hydration method, and their physicochemical properties were characterized. The cellular uptake of the micelles was confirmed by confocal laser scanning microscopy in A549 lung cancer cells and HepG₂ liver cancer cells. In addition, cytotoxicity of the piperine mixed micelles was studied in A549 lung cancer cells and HepG₂ liver cancer cells. Free piperine or piperine-loaded Soluplus^®/TPGS mixed micelles were administered at an equivalent dose of piperine at 3.2?mg/kg via a single intravenous injection in the tail vain for the pharmacokinetic study in vivo.

Results: The diameter of piperine-loaded Soluplus^®/TPGS (4:1) mixed micelles was about 61.9?nm and the zeta potential –1.16?±?1.06?mV with 90.9% of drug encapsulation efficiency and 4.67% of drug-loading efficiency. Differential scanning calorimetry (DSC) studies confirmed that piperine is encapsulated by the Soluplus^®/TPGS. The release results in vitro showed that the piperine-loaded Soluplus^®/TPGS mixed micelles presented sustained release behavior compared to the free piperine. The mixed micelles exhibited better antitumor efficacy compared to free piperine and physical mixture against in A549 and HepG₂ cells by MTT assay. The pharmacokinetic study revealed that the AUC of piperine-loaded mixed micelles was 2.56 times higher than that of piperine and the MRT for piperine-loaded mixed micelles was 1.2-fold higher than piperine (p?Conclusion: The results of the study suggested that the piperine-loaded mixed micelles developed might be a potential nano-drug delivery system for cancer chemotherapy. These results demonstrated that piperine-loaded Soluplus^®/TPGS mixed micelles are an effective strategy to deliver piperine for cancer therapy.     

Nifedipine in semi-solid formulations for topical use in peripheral vascular disease: preparation,characterization, and permeation assay

Nifedipine (NFD) has been used for the treatment of cutaneous lesions caused by peripheral vascular disease and diabetic ulcers. NFD was formulated at 8% in three semi-solid formulations: Polaxamer 407 Lecithin Organogel (PLO), PLO plus Transcutol^®, and an oil-in-water (o/w) emulsion. In vitro release and permeation tests were carried out using a synthetic (cellulose acetate) or natural membrane (pig ear skin), respectively, mounted in a Franz-type diffusion cell at 37°C in a constant water bath. As a receptor solution, isotonic phosphate buffer at pH 7.4 was used. All samples were analyzed by high-performance liquid chromatography by employing a previously validated method. The drug flow values were 6.126?±?0.288, 4.030?±?0.081, and 6.660?±?0.254 μg/cm²/h for PLO, PLO plus Transcutol^®, and o/w emulsion, respectively. The three formulations did not show significant differences in drug flow, considering p > 0.05. Furthermore, their penetration profiles in both the epidermis and dermis were statistically different. Thus, the incorporation of NFD in PLO, PLO plus Transcutol^®, and o/w emulsion changed the drug thermodynamic activity, as expected. In addition, Transcutol^® increased the solubility of NFD in the formulation and promoted its penetration in both the epidermis and dermis.     

Facile development,characterization, and optimization of new metformin-loaded nanocarrier system for efficient colon cancer adjunct therapy

Purpose: Metformin hydrochloride (MF) repurposing as adjuvant anticancer therapy for colorectal cancer (CRC) proved effective. Several studies attempted to develop MF-loaded nanoparticles (NPs), however the entrapment efficiency (EE%) was poor. Thus, the present study aimed at the facile development of a new series of chitosan (CS)-based semi-interpenetrating network (semi-IPN) NPs incorporating Pluronic^® nanomicelles as nanocarriers for enhanced entrapment and sustained release of MF for efficient treatment of CRC.

Methods: The NPs were prepared by ionic gelation and subsequently characterized using FTIR, DSC, TEM, and DLS. A full factorial design was also adopted to study the effect of various formulation variables on EE%, particle size, and zeta-potential of NPs.

Results: NPs had a spherical shape and a mean particle size ranging between 135 and 220?nm. FTIR and DSC studies results were indicative of successful ionic gelation with the drug being dispersed in its amorphous form within CS-Pluronic^® matrix. Maximum EE% reaching 57.00?±?12.90% was achieved using Pluronic^®-123 based NPs. NPs exhibited a sustained release profile over 48?h. The MF-loaded NPs sensitized RKO CRC cells relative to drug alone.

Conclusion: The reported results highlighted the novel utility of the developed NPs in the arena of colon cancer treatment.     

Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients

The aim of this study was to prepare fast-disintegrating tablets (FDTs) of diclofenac potassium with sufficient integrity as well as a pleasant taste, using two different fillers and binders: Tablettose 70® and Di-Pac^®. Tablets were made with direct compression method. Tablet properties such as porosity, hardness, and disintegration time were determined. Diclofenac potassium determinations were carried out using a validated spectrophotometric method for the analysis of drug. Furthermore, in vivo experiments were carried out to compare the analgesic effect and the time to relieve migraine headache between the commercial tablets and FDTs of diclofenac potassium against placebo. Results showed that FDTs of diclofenac potassium with durable structure and desirable taste can be prepared using both fillers and binders but tablets prepared with Di-Pac had a better taste so the tablet formulation containing Di-Pac was chosen for in vivo experiments. Placebo controlled in vivo trial demonstrated that 50 mg diclofenac potassium, administered as a single dose of FDTs or commercial tablets, was effective in relieving the pain and both of them were superior to placebo.     

Effect of Kollidon VA®64 particle size and morphology as directly compressible excipient on tablet compression properties

The study evaluates use of Kollidon VA^®64 and a combination of Kollidon VA^®64 with Kollidon VA^®64 Fine as excipient in direct compression process of tablets. The combination of the two grades of material is evaluated for capping, lamination and excessive friability. Inter particulate void space is higher for such excipient due to the hollow structure of the Kollidon VA^®64 particles. During tablet compression air remains trapped in the blend exhibiting poor compression with compromised physical properties of the tablets. Composition of Kollidon VA^®64 and Kollidon VA^®64 Fine is evaluated by design of experiment (DoE). A scanning electron microscopy (SEM) of two grades of Kollidon VA^®64 exhibits morphological differences between coarse and fine grade. The tablet compression process is evaluated with a mix consisting of entirely Kollidon VA^®64 and two mixes containing Kollidon VA^®64 and Kollidon VA^®64 Fine in ratio of 77:23 and 65:35. A statistical modeling on the results from the DoE trials resulted in the optimum composition for direct tablet compression as combination of Kollidon VA^®64 and Kollidon VA^®64 Fine in ratio of 77:23. This combination compressed with the predicted parameters based on the statistical modeling and applying main compression force between 5 and 15?kN, pre-compression force between 2 and 3?kN, feeder speed fixed at 25?rpm and compression range of 45–49?rpm produced tablets with hardness ranging between 19 and 21?kp, with no friability, capping, or lamination issue.     

Application of hot melt extrusion for improving bioavailability of artemisinin a thermolabile drug

Hot melt extrusion has been used to produce a solid dispersion of the thermolabile drug artemisinin. Formulation and process conditions were optimized prior to evaluation of dissolution and biopharmaceutical performance. Soluplus^®, a low T_g amphiphilic polymer especially designed for solid dispersions enabled melt extrusion at 110?°C although some drug-polymer incompatibility was observed. Addition of 5% citric acid as a pH modifier was found to suppress the degradation. The area under plasma concentration time curve (AUC_0–24h) and peak plasma concentration (C_max) were four times higher for the modified solid dispersion compared to that of pure artemisinin.     

Effect of polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets

Abstract

The present study involved the design and development of oral bioadhesive pellets of eplerenone. A solid dispersion of eplerenone was developed with a hydrophilic carrier, polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (Soluplus^®). Bioadhesive pellets were prepared from this solid dispersion using a combination of HPMC K4M and Carbopol 934P. Both the solid dispersion and the pellets were evaluated for various physicochemical properties such as solubility, entrapment efficiency, drug content, surface morphology, mucoadhesion and swelling behavior. Analysis carried out using FT-IR, DSC and XRD found no interaction between the eplerenone and excipients. The solid dispersion had irregular-shaped smooth-surfaced particles of diameter 265?±?105.5?μm. In TEM analysis, eplerenone particles of size 79–120?nm were found. The solubility and dissolution of eplerenone in the Soluplus^®-based solid dispersion were 5.26 and 2.50 times greater, respectively. Investigation of the swelling behavior of the pellets showed that the thickness of the gel layer increased continuously over the duration of the study. Moreover, a correlation was observed between the thickness and strength of the gel layer and the percentage release. The mechanism of drug release was found to be non-Fickian (anomalous), with the release kinetics approaching first-order kinetics. The bioavailability of the eplerenone bioadhesive pellet formulation was studied using Wistar rats and was found to be improved. An in vivo mucoadhesion study showed that the pellets are retained for 24?h in rabbits. It was concluded that Soluplus^® had a positive effect on the solubility and dissolution of pellets without affecting the bioadhesion.     

Preparation and evaluation of self-assembly Soluplus®-sodium cholate-phospholipid ternary mixed micelles of docetaxel

Abstract

Ternary mixed micelles constituted of Soluplus^®, sodium cholate, and phospholipid were prepared as nano-delivery system of the anticancer drug, docetaxel. The formulation of docetaxel-loaded ternary mixed micelles (DTX-TMMs) with an optimized composition (Soluplus^®/sodium cholate/phospholipid= 3:2:1 by weight) were obtained. The main particle size of DTX-TMMs was 76.36?±?2.45?nm, polydispersity index (PDI) was 0.138?±?0.039, and the zeta potential was ?8.46?±?0.55?mv. The encapsulation efficiency was 94.24?±?4.30% and the drug loading was 1.25%. The critical micelle concentration value was used to assess the ability of carrier materials to form micelles. The results indicated that the addition of Soluplus^® to sodium cholate-phospholipid mixed micelles could reduce the critical micelle concentration and improve the stability. In vitro release studies demonstrated that compared with DTX-Injection group, the DTX-TMMs presented a controlled release property of drugs. In vivo pharmacodynamics results suggested that DTX-TMMs had the most effective inhibitory effect on tumor proliferation and had good biosafety. In addition, the relative bioavailability of mixed micelles was increased by 1.36 times compared with the DTX-Injection in vivo pharmacokinetic study indicated that a better therapeutic effect could be achieved. In summary, the ternary mixed micelles prepared in this study are considered to be promising anticancer drug delivery systems.     

Comparison between the fatigue response of hot and warm mix asphalts based on the dissipated energy approach

This study focused on the fatigue behaviour of warm mix asphalt (WMA) based on the dissipated energy (DE) approach. Two conventional binders consisting of 60/70 and 85/100 penetration-grade bitumens were used to prepare the control mix. WMA was prepared by incorporating 2% Sasobit by weight of bitumen. First, the basic properties of WMA containing optimum bitumen content were compared with those of control hot mix asphalt (HMA). The main laboratory programme included four-point flexural fatigue test that was accomplished at different strain levels of 250, 500, 750 and 1000 microstrain. The studied WMA had comparable Marshall stability and indirect tensile strength to those of control HMA. Furthermore, based on the resilient modulus test results, the temperature susceptibility of WMA was slightly more than that of the control mix. Fatigue lives of studied mixes were evaluated using the conventional fatigue curves that were developed based on the initial strain level. Comparison between these curves revealed the predominant fatigue behaviour of WMAs at different examined strain levels. The initial DE and the cumulative DE of WMAs were lower than those of HMAs. The latter issue justifies the predominant fatigue response of WMA. By considering the DE curve, the ratio of dissipated energy change (RDEC) was calculated. Afterward, the plateau value (PV) was determined using the moving average of fatigue data in the plateau stage of the RDEC curve. Finally, PV-based fatigue models were developed which could precisely estimate the fatigue life regardless of the mix type and testing condition.     

Preparation,characterization, and pharmacokinetics study of a novel genistein-loaded mixed micelles system

Genistein (GEN), is a natural dietary isoflavone, has been reported to show anticancer activities. However, its poor aqueous solubility and oral bioavailability limit its clinical application. We designed a novel genistein-loaded mixed micelles (GEN-M) system composed of Soluplus^® and Vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were prepared by organic solvent evaporation aimed to overcome the challenges of GEN’s poor solubility and then further improve its oral bioavailability. The optimized, spherical-shaped GEN-M was obtained at a ratio of 10:1 (Soluplus^®:TPGS). The mean particle size of GEN-M was 184.7?±?2.8?nm, with a narrow polydispersity index (PDI) of 0.162?±?0.002. The zeta potential value of GEN-M was ?2.92?±?0.01?mV. The micelles solutions was transparent with blue opalescence has high the entrapment efficiency (EE) and drug loading (DL) of 97.12?±?2.11 and 3.87?±?1.26%, respectively. GEN-M was demonstrated a sustained release behavior when formed micelles shown in drug release in vitro. The solubility of GEN in water increased to 1.53?±?0.04?mg/mL after encapsulation. The permeability of GEN across a Caco-2 cell monolayer was enhanced, and the pharmacokinetics study of GEN-M showed a 2.42-fold increase in relative oral bioavailability compared with free GEN. Based on these findings, we conclude that this novel nanomicelles drug delivery system could be leveraged to deliver GEN and other hydrophobic drugs.