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Myricetin (MYR) was incorporated into pH-sensitive liposomes in order to improve its bioavailability and anti-hyperuricemic activity. The MYR pH-sensitive liposomes (MYR liposomes) were prepared using thin film dispersion method, and assessed by particle size (PS), polydispersed index (PDI), zeta potential (ZP), encapsulation efficiency, drug loading, and in vitro release rate. Pharmacokinetics and anti-hyperuricemic activities were also evaluated. The PS, PDI, ZP, encapsulation efficiency, and drug loading of MYR liposomes were 184.34 ± 1.05 nm, 0.215 ± 0.005, −38.46 ± 0.30 mV, 83.42 ± 1.07%w/w, and 6.20 ± 0.31%w/w, respectively. The release rate of MYR liposomes was higher than free MYR, wherein the cumulative value responded to pH. Besides, the Cmax of MYR liposomes was 4.92 ± 0.20 μg/mL. The level of uric acid in the M-L-H group (200 mg/kg) was reduced by 54.74%w/v in comparison with the model group. MYR liposomes exhibited pH sensitivity and could potentially enhance the oral bioavailability and anti-hyperuricemic efficacy of MYR. [ABSTRACT FROM AUTHOR]

To prepare polyethylene glycol succinate-vitamin E modified pinocembrin (PCB)-loaded liposomes (PCBT-liposomes) and evaluate PCBT-liposomal pharmacokinetics and antihyperglycemic activity. The novel PCBT-liposomes demonstrated a promising application prospect as a nano drug carrier for future research. Thin film dispersion was used to prepare PCBT-liposomes. We measured a series of characterization, followed by in vitro cumulative release, in vivo pharmacokinetic study, and antihyperglycemic activity evaluation. PCBT-liposomes displayed spherical and bilayered nanoparticles with mean particle size (roughly 92 nm), negative zeta potential (about −26.650 mV), high drug encapsulation efficiency (87.32 ± 1.34%) and good storage (at 4 or 25 °C) stability during 48 h after hydration. The cumulative release rate of PCBT-liposomes was markedly higher than free PCB in four different pH media. In vivo investigation showed that PCBT-liposomes could obviously improve oral bioavailability of PCB by 1.96 times, whereas the Cmax, MRT0–t, and T1/2 of PCBT-liposomes were roughly 1.700 ± 0.139 µg·mL−1, 12.695 ± 1.647 h, and 14.244 h, respectively. In terms of biochemical analysis, aspartate amino-transferase (AST), alanine amino-transferase (ALT), interleukin-1 (IL-1), and tumor necrosis factor-α (TNF-α) concentrations in serum of diabetic mice were respectively decreased 28.28%, 17.23%, 17.77%, and 8.08% after PCBT-liposomal treatment. These results show PCBT-liposomal preparation as an excellent nano-carrier which has the potential to improve water solubility, bioavailability, and antihyperglycemic activity of PCB, amid broadening the application of PCB in the clinical settings. [ABSTRACT FROM AUTHOR]

Due to the obstruction and heterogeneity of the blood-brain barrier, the clinical treatment of glioma has been extremely difficult. Isoliquiritigenin (ISL) exhibits antitumor effects, but its low solubility and bioavailability limit its application potential. Herein, we established a nanoscale hybrid membrane-derived system composed of erythrocytes and tumor cells. By encapsulating ISL in hybrid membrane nanoparticles, ISL is expected to be enhanced for the targeting and long-circulation in gliomas therapy. We fused erythrocytes with human glioma cells U251 and extracted the fusion membrane via hypotension, termed as hybrid membrane (HM). HM-camouflaged ISL nanoparticles (ISL@HM NPs) were prepared and featured with FT-IR, SEM, TEM, and DLS particle analysis. As the results concluded, the ISL active pharmaceutical ingredients (APIs) were successfully encapsulated with HM membranes, and the NPs loading efficiency was 38.9 ± 2.99% under maximum entrapment efficiency. By comparing the IC50 of free ISL and NPs, we verified that the solubility and antitumor effect of NPs was markedly enhanced. We also investigated the mechanism of the antitumor effect of ISL@HM NPs, which revealed a marked inhibition of tumor cell proliferation and promotion of senescence and apoptosis of tumor cells of the formulation. In addition, the FSC and WB results examined the effects of different concentrations of ISL@HM NPs on tumor cell disruption and apoptotic protein expression. Finally, it can be concluded that hybridized membrane-derived nanoparticles could prominently increase the solubility of insoluble materials (as ISL), and also enhance its targeting and antitumor effect. [ABSTRACT FROM AUTHOR]

Hyperoside (Hyp) self-assembled polymeric micelles (Hyp-PMs) were purposely developed to enhance aqueous solubility, in vivo availability and anti-oxidative effect of Hyp. In preparing Hyp-PMs, we employed the thin film dispersion method with the micelles consisting of TPGs and mPEG2000-PDLLA3000. The particle size, polydispersity index and zeta potential of Hyp-PMs were 67.42 ± 1.44 nm, 0.229 ± 0.015 and −18.67 ± 0.576 mV, respectively, coupled with high encapsulation efficiency （EE）of 90.63 ± 1.45% and drug loading (DL) of 6.97 ± 1.56%. Furthermore, the value of critical micelle concentration (CMC) was quite low, which indicated good stability and improved self-assembly ability of Hyp-PMs. Also, trend of in vitro Hyp release from Hyp-PMs demonstrated enhanced solubility of Hyp. Similarly, in comparison with free Hyp, oral bioavailability of Hyp-PMs was improved (about 8 folds) whilst half-life of Hyp-PMs was extended (about 3 folds). In vitro anti-oxidative effect showed obvious strong scavenging DPPH capability of Hyp-PMs, which may be attributed to its smaller size and better solubility. Altogether, Hyp-PMs may serve as a possible strategy to potentially enhance aqueous solubility, bioavailability and anti-oxidative effect of Hyp, which may play a key role in Hyp application in the pharmaceutical industries. [ABSTRACT FROM AUTHOR]

The pharmacological activities of liquiritin (LT) are greatly limited by its insolubility and low oral absorption. The purpose of this study was to prepare LT-hydroxypropyl-beta-cyclodextrin inclusion complex (LT-HP-β-CD) to increase water solubility, oral bioavailability and antitumor effect of LT. Herein, saturated aqueous solution method was applied to prepare the LT-HP-β-CD prior to characterization via scanning electron microscope (SEM), infrared radiation (IR) spectroscopy, X-ray diffraction analysis (XRD), and differential scanning calorimetry (DSC). Also, in vitro release and in vivo pharmacokinetics were evaluated. Moreover, the anti-tumor activity of the formulation was investigated in the A549 lung cancer cells. The results of SEM, IR, XRD and DSC showed that LT-HP-β-CD was successfully formulated. In vitro release and oral bioavailability of LT-HP-β-CD compared with the free LT was significantly higher. Successfully, antitumor effect of LT was remarkably enhanced by the preparation of LT-HP-β-CD. Altogether, the LT-HP-β-CD represents a potential carrier for enhancing the water solubility and oral bioavailability of LT coupled with antitumor activity enhancement. [Display omitted] [ABSTRACT FROM AUTHOR]

BACKGROUND This study focused on the development of a self‐nanoemulsifying drug delivery system (SNEDDS) to improve, potentially, the solubility and oral bioavailability of liquiritin (LQ). METHODS: The solubility of LQ in different types of excipient, namely oils (OLs), emulsifiers (EMs), and co‐emulsifiers (CO‐EMs), was evaluated, and a pseudo‐ternary phase diagram (PTPD) and the formulation optimization were established. The prepared self‐nanoemulsifying drug delivery system of liquiritin (LQ‐SNEDDS) was assessed using droplet size (DS), zeta potential (ZP), polydispersity index (PDI), droplet morphology, drug release in vitro, and oral bioavailability. RESULTS: After the dilution of the LQ‐SNEDDS, a transparent nanoemulsion was obtained with an acceptable DS (24.70 ± 0.73 nm), ZP (−18.69 ± 1.44 mV), and PDI (0.122 ± 0.006). The LQ‐SNEDDS that was developed had a better release rate in vitro than the free LQ suspension. Pharmacokinetic evaluation showed that the relative oral bioavailability of LQ‐SNEDDS was increased by 5.53 times, and LQ‐SNEDDS exhibited a delayed half life and longer retention time in comparison with those of free LQ. Similarly, LQ‐SNEDDS had a better urate lowering effect and provided better organ protection than free LQ at the same dose (P < 0.05). CONCLUSIONS: The incorporation of LQ into SNEDDS could serve as a promising approach to improve the solubility, oral bioavailability, and anti‐hyperuricemic effect of LQ. © 2021 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

A liposome of Licochalcone A (LCA‐Liposomes) was purposively prepared to ameliorate the low in vivo availability and efficacy of LCA. Physical characterization of LCA‐Liposomes was carried out mainly by determining particle size, morphology, zeta potential (Z‐potential), and efficiency of LCA encapsulation (EE) via appropriate techniques. Also, the rate of LCA release in vitro and distribution in vivo (plasma and tissues) was evaluated. Evaluation of the antirenal activity of LCA‐liposomes was carried out by establishing chronic renal failure (CRF) model in mice through intragastric administration of adenine (200 mg/kg) and subsequent determination of biochemical parameters and examination of tissue sections. Respectively, the mean size of liposomal particles, Z‐potential and EE of LCA‐Liposomes were 71.78 ± 0.99 nm, −38.49 ± 0.06 mV, and 97.67 ± 1.72%. Pharmacokinetic and tissue distribution studies showed that LCA‐Liposomes could improve the availability of LCA in the blood and tissues, whereas during pharmacodynamics studies, the liposome effectively improved the therapeutic effect of LCA on CRF mice by potentially protecting the renal tissues while exhibiting antioxidant activity. In conclusion, LCA‐Liposomes could effectively improve the bioavailability of LCA and provide platform for the development of LCA‐related functional products. Practical applications: As a traditional Chinese medicine, licorice is widely used in food and pharmaceutical industries. LCA is a small molecule flavonoid extracted from the root of licorice. In this study, LCA was loaded on liposome carriers, which significantly improved the water solubility and oral bioavailability, and proved that LCA‐Liposomes have certain therapeutic effects on chronic renal failure, thereby providing a basis for the development of LCA into drugs or functional food in the future. [ABSTRACT FROM AUTHOR]

The aim of this study was to develop licochalcone A-loaded self-microemulsifying drug delivery system (LCA-SMEDDS) to improve bioavailability and anti-hyperuricemic activity of hydrophobic natural compound licochalcone A (LCA). The prepared LCA-SMEDDS was characterised by transmission electron microscopy analysis, particle size, polymer dispersity index (PDI), zeta potential, stability tests and in vitro release analysis. LCA-SMEDDS and free LCA were orally administered to Sprague-Dawley rats to investigate respective bioavailability. The hyperuricaemia rat model was established to evaluate anti-hyperuricemic activity. The particle size, PDI, and zeta potential of LCA-SMEDDS were 25.68 ± 0.79 nm, 0.074 ± 0.024, −14.37 ± 2.17 mV. The oral bioavailability of LCA-SMEDDS was increased 2.36-fold compared with the free LCA. The uric acid level of LCA-SMEDDS group (200 mg/kg) was decreased 60.08% compared with model control group. The developed LCA-SMEDDS could be an outstanding candidate for improving oral bioavailability and anti-hyperuricemic activity of LCA. [ABSTRACT FROM AUTHOR]

Herein, a nano-micelle drug delivery system was developed to orally improved zingerone's bioavailability and its antitumor effect. Indeed, zingerone-loaded d-α-tocopheryl polyethylene glycol succinate micelles (ZTMs) were effectively prepared, characterised and assessed. The ZTMs had diameter, polydispersity index, and zeta potential of 50.62 ± 0.25 nm, 0.168 ± 0.006, and −28.07 ± 0.33 mV, respectively, coupled with a high entrapment efficiency (m/m, %) were 94.71 ± 2.02. The release rate of ZTMs in three media was significantly greater than that of free zingerone. Intriguingly, results obtained from pharmacokinetic studies showed that the oral bioavailability of the ZTMs was enhanced by 5.10 times in comparison with the free zingerone. Further, the half inhibitory concentration (IC50) of ZTMs and free zingerone was 7.56 μg/ml and 14.30 μg/ml, respectively, on HepG2 cells. Hence, ZTMs may be used as a potential approach to enrich the solubility, bioavailability, and concomitant anti-proliferative effect of zingerone in vitro. [ABSTRACT FROM AUTHOR]

Liquiritin, as one of the main flavonoids in Glycyrrhiza, exhibits extensive pharmacological effects, such as the anti-oxidant, anti-inflammatory, anti-tumor and so on. Herein, the aqueous solubility and oral bioavailability of liquiritin was purposely enhanced via the preparation of the mixed micelles. The liquiritin-loaded micelles (LLM) were fabricated via thin-film dispersion method. The optimal LLM formulation was evaluated through physical properties including particle size (PS), encapsulation efficiency (EE) and drug loading (DL). In vitro accumulate release as well as in vivo pharmacokinetics were also evaluated. Moreover, the hypolipidemic activity of LLM was observed in the hyperlipidemia mice model. The LLM exhibited a homogenous spherical shape with small mean PS, good stability and high encapsulation efficiency. The accumulate release rates in vitro of the LLM were obviously higher than free liquiritin. The oral bioavailability of the formulation was heightened by 3.98 times in comparison with the free liquiritin. More importantly, LLM increased the hypolipidemic and effect of alleviating lipid metabolism disorder in hepatocytes of liquiritin in hyperlipidemia mice model. Collectively, the improved solubility of liquiritin in water coupled with its enhanced oral bioavailability and concomitant hypolipidemic activity could be attributed to the incorporation of the drug into the mixed micelles. [ABSTRACT FROM AUTHOR]

6-Gingerol, an active herbal ingredient of ginger has various bioactivities such as anti-neurodegenerative disease, anti-inflammatory and so on. The aim of the present study was to enhance the oral bioavailability and brain distribution of 6-Gingerol via polymeric micelles. A polymeric micelles drug delivery system of 6-Gingerol consisting of D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and Poly (ethylene glycol)-poly (ε-caprolactone) (PEG-PCL) was prepared via solvent injection method. The developed 6-Gingerol-loaded TPGS/PEG-PCL micelles (6-GTPMs) were characterized based on particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency (EE), drug loading (DL) and in vitro release profile. The pharmacokinetics and tissue distribution studies were also evaluated. The nanoformulation produced a particle size of 73.24 ± 2.84 nm with acceptable PDI (0.129 ± 0.03), zeta potential (−2.74 ± 0.92 mV), DL (4.64%) and EE (79.68%). The in vitro release profile showed that the 6-GTPMs enhanced the solubility of 6-Gingerol, while the pharmaceutical analysis in rats indicated that 6-GTPMs significantly improved the oral bioavailability of 6-Gingerol (about 3 folds) in circulation. The 6-GTPMs exhibited remarkable brain targetability in the tissue distribution analysis. Collectively, a 6-Gingerol polymeric micelle with enhanced oral bioavailability coupled with excellent brain distribution was successfully developed. [ABSTRACT FROM AUTHOR]

Graphical abstract Abstract [6]-Shogaol, an alkylphenol compound purified from the root and stem of ginger (Zingiber officinale), has attracted considerable interest due to its potential anticancer, antioxidative and antirheumatic properties. However, the oral bioavailability of [6]-shogaol has been severely limited because of its poor solubility. In this study, a significant quantity of high-purity [6]-shogaol (yield: 3.6%; purity: 98.65%) was extracted and encapsulated in solid lipid nanoparticles (SLNs) via high-pressure homogenization (encapsulation efficiency: 87.67%) to improve its solubility and oral bioavailability. The resulting [6]-shogaol-loaded solid lipid nanoparticles (SSLNs) were stable, homogeneous and well-dispersed. Its mean particle size and zeta potential were 73.56 ± 5.62 nm and −15.2 ± 1.3 mV, respectively. Importantly, the in vitro release profile and in vivo oral bioavailability of SSLNs were significantly improved compared with the free drug. Furthermore, the SSLNs could remarkably lower the uric acid level via inhibiting the activity of xanthine oxidase and reduce the production of interleukin-1β (IL-1β) and tumor necrosis factor (TNF-α) in the hyperuricemia/gouty arthritis rat model, when compared to the free [6]-shogaol. Collectively, SLNs could serve as a promising drug delivery system to improve the oral bioavailability of [6]-shogaol for effective treatment of gouty arthritis. [ABSTRACT FROM AUTHOR]

[6]-Gingerol, one of the components of the rhizome of Ginger, has a variety of biological activities such as anticoagulant, antioxidative, antitumor, anti-inflammatory, antihypertensive, and so forth. However, as one of the homologous phenolic ketones, [6]-gingerol is insoluble in water which limits its applications. Herein, we prepared [6]-gingerol proliposomes through modified thin-film dispersion method, which was spherical or oval, and physicochemically stable with narrow size distribution. Surprisingly, in vitro release of [6]-gingerol loaded proliposome compared with the free [6]-gingerol was significantly higher and its oral bioavailability increased 5-fold in vivo. Intriguingly, its antitumor effect was enhanced in the liposome formulation. Thus, our prepared [6]-gingerol proliposome proved to be a novel formulation for [6]-gingerol, which significantly improved its antitumor effect. [ABSTRACT FROM AUTHOR]

The purpose of this study was to develop a [6]-Gingerol-loaded self-microemulsifying drug delivery system ([6]-Gingerol-SMEDDS) for oral administration and enhanced bioavailability of the drug. The [6]-Gingerol-SMEDDS, consisting of oils (ethyl oleate), surfactant (Cremophor EL35) and co-surfactant (1,2-propanediol), showed an acceptable spherical nanoparticle with stable physicochemical properties such as the mean droplet size (73.06 ± 0.49 nm), zeta potential (−2.45 ± 0.41) and encapsulation efficiency (89.40 ± 1.11%). The in vitro release of [6]-Gingerol from the delivery system in the three different media (HCl, pH 1.2; Double distilled water, pH 7.0; phosphate buffer solution, pH 7.4) was significantly higher than in the free drug. The [6]-Gingerol-SMEDDS also exhibited prolonged plasma circulation which led to 6.58-fold increase in oral bioavailability compared with the free drug. These findings indicated that the developed [6]-Gingerol-SMEDDS could be a promising alternative in improving the solubility and oral bioavailability of [6]-Gingerol, as well as increasing its biological applications. [ABSTRACT FROM AUTHOR]

In the present study, a novel nonionic surfactant vesicles (NSVs) system consisting of cholesterol, Tween 80 and Span 80 was developed for the delivery of Ginsenoside Rb 1 with an improved oral bioavailability. The prepared vesicles were hollow and spherically shaped with acceptable diameter (264.68 ± 4.17 nm), zeta potential (−11.58 ± 0.87 mV) and encapsulation efficiency (69.034 ± 0.045%). XRD analysis provided affirmed the encapsulation of Rb 1 in the vesicles. The in vitro release profile of Rb 1 from the vesicles in the two different media (double distilled water, pH 7.0, phosphate buffer solution, pH 7.4) showed statistical insignificant difference when compared with the free Ginsenoside Rb 1. Notably, the pharmacokinetic analysis of optimized Ginsenoside Rb 1 -NSVs exhibited a higher C max (9.55 ± 0.5 μg/mL versus 6.22 ± 0.53 μg/mL) with 1.82-fold increase in relative oral bioavailability. Collectively, these findings revealed that the developed vesicles could be a novel alternative in improving the oral bioavailability of Ginsenoside Rb 1 and extending its application in the clinical setting. [Display omitted] • Ginsenoside Rb 1 was purified from Panax Ginseng extract. • Oral bioavailability of Ginsenoside Rb 1 was improved after encapsulation in vesicles. [ABSTRACT FROM AUTHOR]

The purpose of this study was to develop a precursor liposome nano-delivery system for liquiritin (LT) to improve its solubility, oral bioavailability, and efficacy. The characterizations of the particle diameter, zeta potential, polydispersity index (PDI), droplet morphology, drug release in vitro , and oral bioavailability of the prepared LT precursor liposomes (LTMs) were carried out. In addition, streptozotocin intraperitoneal injection successfully induced diabetic mouse model, while the LT hypoglycemic effect, oral glucose tolerance, biochemical parameters and pathological sections were studied. The prepared LTMs were diluted to obtain a clear and transparent solution with a diameter of 91.84 ± 1.85 nm, zeta potential of −38.59 ± 2.65 mV and PDI of 0.215 ± 0.016. The in vitro release of the LTMs was superior to that of the free LT suspension, which may be related to the increased solubility of LT, as well as the small diameter and increased surface area. The obtained pharmacokinetic parameters indicated that the relative oral bioavailability of LTMs was increased by 8.8 times compared with the free LT suspension. Pharmacodynamic studies showed that LTMs effectively improved LT's hypoglycemic effect and diabetes-related organ repair, simultaneously confirmed its antioxidant activity. These results implied that the LTMs was an effective method to improve the solubility, oral bioavailability, and hypoglycemic activity of LT. [ABSTRACT FROM AUTHOR]

In this study, we sought to overcome the poor solubility and bioavailability of bismethoxycurcumin (BDMC) by fabricating a BDMC-loaded self micro-emulsifying system (BDMC-SMEDDS). Solubility and compatibility tests, pseudo-ternary phase diagrams (PTPDs) as well as d-optimal concept was applied to design the formulation. The assessment of the prepared BDMC-SMEDDS in-vitro mainly included droplet size (DS) and entrapment efficiency (EE) determination, morphology, drug release and stability testing. Besides, the in vivo behavior was also evaluated after oral administration of BDMC-SMEDDS to rats. The optimal formulation was found to compose of Kolliphor EL (K-EL, emulsifier, 645.3 mg), PEG 400 (co-emulsifier, 147.2 mg), ethyl oleate (EO, oil, 207.5 mg) and BDMC (50 mg). The BDMC-SMEDDS with satisfactory stability had a mean size of 21.25 ± 3.23 nm and EE of 98.31 ± 0.32%. Roughly 70% of BDMC was released from BDMC-SMEDDS within 84 h compared with <20% from the free BDMC. More importantly, the in-vivo behavior of BDMC-SMEDDS showed that the AUC (0-12h) and plasma concentration of BDMC increased substantially as compared to the free BDMC. Altogether, BDMC-SMEDDS has the potential to enhance the solubility and bioavailability of BDMC and could be applied in the clinics. [ABSTRACT FROM AUTHOR]

Myricitrin has many pharmacological effects, such as anti-inflammation, liver protection and anti-oxidation. However, its clinical application is limited by poor solubility and low oral bioavailability. The preparation of myricitrin-loaded proliposomes (MPs) was achieved via the combination of thin-film dispersion technique and freeze-drying method. The in vitro release of MPs compared with free myricitrin was measured in different dissolution media while the pharmacokinetic study was also conducted in rats. Moreover, the uric acid-lowering activity of MPs was investigated in the hyperuricemic rat model. The prepared myricitrin appeared to be spherical. Notably, compared with the free myricitrin, the cumulative release in vitro and in vivo oral bioavailability of MPs were markedly increased. Besides, the MPs could significantly lower the serum uric acid level as well as ameliorate liver and kidney damage in hyperuricemic rats compared with the model group. Therefore, the present work supports the fact that MPs improved the oral bioavailability of myricitrin for the prospect of clinical application. [ABSTRACT FROM AUTHOR]

6-shogaol is a promising anti-cancer and anti-inflammatory agent. However, the treatment effectiveness of 6-shogaol is limited by poor water solubility, poor oral absorption and rapid metabolism. Herein, 6-shogaol loaded in micelles (SMs) were designed to improve 6-shogaol's solubility and bioavailability. The micelles of a PEG derivative of linoleic acid (mPEG2k-LA) were prepared by the nanoprecipitation method with a particle size of 76.8 nm, and entrapment of 81.6 %. Intriguingly, SMs showed a slower release in phosphate buffer saline (PBS) (pH = 7.4) compared to free 6-shogaol while its oral bioavailability increased by 3.2–fold in vivo. More importantly, the in vitro cytotoxic effect in HepG2 cells of SMs was significantly higher than free 6-shogaol. Furthermore, SMs could significantly improve the tissue distribution of 6-shogaol, especially liver and brain. Finally, SMs showed a better hepatoprotective effect against carbon tetrachloride (CCl4)-induced hepatic injury in vivo than free 6-shogaol. These results suggest that the novel micelles could potentiate the activities of 6-shogaol in cancer treatment and hepatoprotection. [ABSTRACT FROM AUTHOR]

Despite its low water solubility, esculetin (EC) have been described to demonstrate various health benefits. Thus, we sought to develop esculetin-loaded mixed micelles (EC-M) delivery system to purposively improve biological availability and anti-hyperglycemia activity of EC. Thin-film hydration method was employed to fabricate EC-M, amid characterization with transmission electron microscopic analysis (TEM), coupled with physical properties such as particle size (PS), poly-dispersity index (PDI), zeta-potential (ZP) and stability testing. We analyzed in-vitro release and studied EC-M pharmacokinetics in rats. The hyperglycemic mice model was established with streptozotocin (STZ) to evaluate anti-hyperglycemic activity of EC-M. The PS, PDI and ZP of EC-M were 47.97 ± 0.41 nm, 0.189 ± 0.005 and -25.55 ± 0.28 mV, respectively. The release rate of EC-M increased comparable to free EC in the three media. The oral biological availability and half-life of EC-M increased respectively by 3.06 and 1.45 folds compared to free EC. Besides, we observed 46.21% decrease in blood glucose of mice in EC-M group comparable to the model control, wherein, the anti-hyperglycemic effect of EC-M was better compared to free EC. Conclusively, EC-M may ideally serve as a novel approach to enhance biological availability and increased anti-hyperglycemic activity of EC. [ABSTRACT FROM AUTHOR]