Delivery Strategies of siRNA Therapeutics for Hair Loss Therapy.

Therapeutic needs for hair loss are intended to find small interfering ribonucleic acid (siRNA) therapeutics for breakthrough. Since naked siRNA is restricted to meet a druggable target in clinic,, delivery systems are indispensable to overcome intrinsic and pathophysiological barriers, enhancing targetability and persistency to ensure safety, efficacy, and effectiveness. Diverse carriers repurposed from small molecules to siRNA can be systematically or locally employed in hair loss therapy, followed by the adoption of new compositions associated with structural and environmental modification. The siRNA delivery systems have been extensively studied via conjugation or nanoparticle formulation to improve their fate in vitro and in vivo. In this review, we introduce clinically tunable siRNA delivery systems for hair loss based on design principles, after analyzing clinical trials in hair loss and currently approved siRNA therapeutics. We further discuss a strategic research framework for optimized siRNA delivery in hair loss from the scientific perspective of clinical translation.

Dataset for hierarchical tetramodal-porous architecture of zinc oxide nanoparticles microfluidically synthesized via dual-step nanofabrication.

Zinc oxide (ZnO) nanoparticles (NPs) have been applied as high-performance intelligent materials to create a hierarchical multimodal-porous architectures for application in biomedical research fields [1]. They were microfluidically synthesized via dual-step nanofabrication compared to the conventional particles including ZnO NPs synthesized at single-pot macroscale, nanosized ZnO, and hybrid ZnO. The physicochemical properties were characterized, including morphology, particle size distribution, atomic composition, crystallinity, purity, reactant viscosity, surface charge, photocatalysis, photoluminescence, and porosity. A hierarchical multimodal-porous three-dimensional (3D) architecture of ZnO NPs was generated and optimized on the solid plate substrate of cellulose paper sheet after solvent evaporation. The dataset provides the nanomaterial design and architecture generation of ZnO NPs, explaining multi-physics phenomena in association with performance optimization processes.

Multiscale Metal Oxide Particles to Enhance Photocatalytic Antimicrobial Activity against Escherichia coli and M13 Bacteriophage under Dual Ultraviolet Irradiation.

Antimicrobial activity of multiscale metal oxide (MO) particles against Escherichia coli (E. coli) and M13 bacteriophage (phage) was investigated under dual ultraviolet (UV) irradiation. Zinc oxide (ZnO), magnesium oxide (MgO), cuprous oxide (Cu2O), and cupric oxide (CuO) were selected as photocatalytic antimicrobials in MO particles. Physicochemical properties including morphology, particle size/particle size distribution, atomic composition, crystallinity, and porosity were evaluated. Under UV-A and UV-C irradiation with differential UV-C intensities, the antimicrobial activity of MO particles was monitored in E. coli and phage. MO particles had nano-, micro- and nano- to microscale sizes with irregular shapes, composed of atoms as ratios of chemical formulae and presented crystallinity as pure materials. They had wide-range specific surface area levels of 0.40-46.34 m2/g. MO particles themselves showed antibacterial activity against E. coli, which was the highest among the ZnO particles. However, no viral inactivation by MO particles occurred in phage. Under dual UV irradiation, multiscale ZnO and CuO particles had superior antimicrobial activities against E. coli and phage, as mixtures of nano- and microparticles for enhanced photocatalytic antimicrobials. The results showed that the dual UV-multiscale MO particle hybrids exhibit enhanced antibiotic potentials. It can also be applied as a next-generation antibiotic tool in industrial and clinical fields.

Antimicrobial Activity of Zinc Oxide Nano/Microparticles and Their Combinations against Pathogenic Microorganisms for Biomedical Applications: From Physicochemical Characteristics to Pharmacological Aspects.

Zinc oxide (ZnO) nano/microparticles (NPs/MPs) have been studied as antibiotics to enhance antimicrobial activity against pathogenic bacteria and viruses with or without antibiotic resistance. They have unique physicochemical characteristics that can affect biological and toxicological responses in microorganisms. Metal ion release, particle adsorption, and reactive oxygen species generation are the main mechanisms underlying their antimicrobial action. In this review, we describe the physicochemical characteristics of ZnO NPs/MPs related to biological and toxicological effects and discuss the recent findings of the antimicrobial activity of ZnO NPs/MPs and their combinations with other materials against pathogenic microorganisms. Current biomedical applications of ZnO NPs/MPs and combinations with other materials are also presented. This review will provide the better understanding of ZnO NPs/MPs as antibiotic alternatives and aid in further development of antibiotic agents for industrial and clinical applications.

In vitro and in vivo toxicological evaluation of transition metal-doped titanium dioxide nanoparticles: Nickel and platinum.

Transition metal-doped titanium dioxide nanoparticles (M-TiO2 NPs) have been studied to enhance the activity of TiO2 NPs in biomedical applications. In this study, in vitro and in vivo toxicological aspects of M-TiO2 NPs were reported to assess the safety of these materials. M-TiO2 NPs were synthesized via a photo-deposition technique. Nickel (Ni) and platinum (Pt) were used as dopants. Physicochemical properties, cytotoxicity, phototoxicity, gene ontology (GO) and dermal toxicity of M-TiO2 NPs were investigated. Ni-TiO2 (Ni, 1.02%) and Pt-TiO2 (Pt, 0.26%) NPs were sphere shape crystals with nanoscale size. ARPE-19 cells were more susceptible to Pt-TiO2 NPs (EC50, 0.796 mg/mL) than Ni-TiO2 NPs (EC50, 2.945 mg/mL). M-TiO2 NPs were rated as probably phototoxic to phototoxic. GO suggested binding function and metabolic processes as a risk mechanism of M-TiO2 NPs. In vivo toxicological effects of Ni-TiO2 NPs were not observed on body weight, serum aspartate transaminase/alanine transaminase levels, and skin histology at 61.5-6150 mg/kg. Specifically, skin thickness was not significantly modified (max. 33.2 ± 8.7 µm) and inflammation grade was less than level 2 (max. 1.2 ± 0.4). From these results, Ni-TiO2 and Pt-TiO2 NPs show promise as enhanced photocatalysts for safe and sustainable usage.

Mass-production and biomarker-based characterization of high-value Spirulina powder for nutritional supplements.

Mass-produced Spirulina powder was characterized based on biomarkers for quality assessment. Other Spirulina powder products for functional foods and animal feeds were used as controls. In this study, Spirulina platensis was mass-cultured in modified Spirulina medium using a dispersive two-ton scale reactor for 30 days. After processing, the Spirulina powder was evaluated using FE-SEM and XPS. In the extracts, chlorophylls were determined using TLC and Q-TOF. SDS-PAGE and DSC were used to analyze protein biomarkers and to monitor thermal stability. The powder presented a microscale distorted sphere. Zinc, iron and calcium were detected on the powder surface. In the extracts, chlorophylls-a, -b, and -c, allophycocyanin, and phycocyanin-C were detected. Despite the similar morphology of all Spirulina products, the mass-produced Spirulina powder showed prolonged protein stability in biochemical compositions. The results suggest that mass-produced Spirulina powder can be characterized using biomarker-based advanced techniques. This protocol can be extended to other microalgae.

Synthesis, Characterization, and Three-Dimensional Structure Generation of Zinc Oxide-Based Nanomedicine for Biomedical Applications.

Zinc oxide (ZnO) nanoparticles have been studied as metal-based drugs that may be used for biomedical applications due to the fact of their biocompatibility. Their physicochemical properties, which depend on synthesis techniques involving physical, chemical, biological, and microfluidic reactor methods affect biological activity in vitro and in vivo. Advanced tool-based physicochemical characterization is required to identify the biological and toxicological effects of ZnO nanoparticles. These nanoparticles have variable morphologies and can be molded into three-dimensional structures to enhance their performance. Zinc oxide nanoparticles have shown therapeutic activity against cancer, diabetes, microbial infection, and inflammation. They have also shown the potential to aid in wound healing and can be used for imaging tools and sensors. In this review, we discuss the synthesis techniques, physicochemical characteristics, evaluation tools, techniques used to generate three-dimensional structures, and the various biomedical applications of ZnO nanoparticles.

Photocatalytic antibacterial application of zinc oxide nanoparticles and self-assembled networks under dual UV irradiation for enhanced disinfection.

BACKGROUND: Zinc oxide (ZnO) nanoparticles and their networks have been developed for use in various applications such as gas sensors and semiconductors. AIM: In this study, their antibacterial activity against Escherichia coli under dual ultraviolet (UV) irradiation for disinfection was investigated. MATERIALS AND METHODS: ZnO nanoparticles were synthesized and immobilized onto silicon (Si) wafers by self-assembly. The physicochemical properties and antibacterial activity of ZnO nanoparticles and their networks were evaluated. Gene ontology was analyzed and toxicity levels were also monitored. RESULTS: Synthesized ZnO nanoparticles were spherical nanocrystals (<100 nm; Zn, 47%; O, 53%) that formed macro-mesoporous three-dimensional nanostructures on Si wafers in a concentration-dependent manner. ZnO nanoparticles and their networks on Si wafers had an excellent antibacterial activity against E. coli under dual UV irradiation (>3log CFU/mL). Specifically, arrayed ZnO nanoparticle networks showed superior activity compared with free synthesized ZnO nanoparticles. Oxidative stress-responsive proteins in E. coli were identified and categorized, which indicated antibacterial activity. Synthesized ZnO nanoparticles were less cytotoxic in HaCaT with an IC50 of 6.632 mg/mL, but phototoxic in Balb/c 3T3. CONCLUSION: The results suggested that ZnO nanoparticles and their networks can be promising photocatalytic antibiotics for use in next-generation disinfection systems. Their application could also be extended to industrial and clinical use as effective and safe photocatalytic antibiotics.

Fabrication of Eudragit polymeric nanoparticles using ultrasonic nebulization method for enhanced oral absorption of megestrol acetate.

Megestrol acetate (MGA) is used as a progestagen to treat advanced cancers in the breast or uterus and anorexia-cachexia syndrome in cancer patients. Due to its low solubility (BCS class II), MGA bioavailability needs to be enhanced for efficacy and safety. We developed MGA-encapsulated Eudragit® L100 (EUD) nanoparticles (MGA-EUD (1:1) and MGA-EUD (2:1)) using an ultrasonic nebulization method. MGA-EUD (1:1) and MGA-EUD (2:1) consisted of MGA and EUD at the mass ratios of 1:1 and 2:1. Their physicochemical properties, i.e. particle size, loading efficiency, morphology, and crystallinity were determined. Dissolution tests were performed using USP method II. For pharmacokinetics, they were orally administered at 50 mg/kg to mice. Microcrystalline MGA suspension (MGA-MC, Megace®, BMS) was used as control. MGA-EUD (1:1) and MGA-EUD (2:1) had a smooth and spherical shape of 0.70 and 1.05 µm in diameter with loading efficiencies of 93 and 95% showing amorphous states of MGA. They significantly enhanced the dissolution potential of MGA. Oral bioavailability of MGA-EUD (1:1) and MGA-EUD (2:1) increased 2.0- and 1.7-fold compared to that of MGA-MC. It suggests that ultrasonic nebulization method for the fabrication of polymeric nanoparticles is a promising approach to improve the bioavailability of poorly soluble drugs.

Dual UV irradiation-based metal oxide nanoparticles for enhanced antimicrobial activity in Escherichia coli and M13 bacteriophage.

Metal oxide (MO) nanoparticles have been studied as nano-antibiotics due to their antimicrobial activities even in antibiotic-resistant microorganisms. We hypothesized that a hybrid system of dual UV irradiation and MO nanoparticles would have enhanced antimicrobial activities compared with UV or MO nanoparticles alone. In this study, nanoparticles of ZnO, ZnTiO3, MgO, and CuO were selected as model nanoparticles. A dual UV collimated beam device of UV-A and UV-C was developed depending upon the lamp divided by coating. Physicochemical properties of MO nanoparticles were determined using powder X-ray diffractometry (PXRD), Brunauer-Emmett-Teller analysis, and field emission-scanning electron microscopy with energy-dispersive X-ray spectroscopy. Atomic force microscopy with an electrostatic force microscopy mode was used to confirm the surface topology and electrostatic characteristics after dual UV irradiation. For antimicrobial activity test, MO nanoparticles under dual UV irradiation were applied to Escherichia coli and M13 bacteriophage (phage). The UV-A and UV-C showed differential intensities in the coated and uncoated areas (UV-A, coated = uncoated; UV-C, coated ≪ uncoated). MO nanoparticles showed sharp peaks in PXRD patterns, matched to pure materials. Their primary particle sizes were less than 100 nm with irregular shapes, which had an 8.6~25.6 m2/g of specific surface area with mesopores of 22~262 nm. The electrostatic properties of MO nanoparticles were modulated after UV irradiation. ZnO, MgO, and CuO nanoparticles, except ZnTiO3 nanoparticles, showed antibacterial effects on E. coli. Antimicrobial effects on E. coli and phages were also enhanced after cyclic exposure of dual UV and MO nanoparticle treatment using the uncoated area, except ZnO nanoparticles. Our results demonstrate that dual UV-MO nanoparticle hybrid system has a potential for disinfection. We anticipate that it can be developed as a next-generation disinfection system in pharmaceutical industries and water purification systems.

Intracorneal melatonin delivery using 2-hydroxypropyl-ß-cyclodextrin ophthalmic solution for granular corneal dystrophy type 2.

Melatonin (MT), an effective antioxidant, has therapeutic implications for granular corneal dystrophy type 2 (GCD2) treatment. Eye drop formulations containing cyclodextrins (CDs) were studied with the objective of improving MT solubility, stability, and ocular absorption, while decreasing eye irritation. MT complexes with αCD, ßCD, γCD, and 2-hydroxypropyl-ßCD (HPßCD) were characterized by phase solubility studies, which demonstrated Higuchi's AL-type phase solubility profiles. The MT/HPßCD complex showed the highest MT solubility (2.75mg/mL). Ocular irritation experiments showed HPßCD inclusion alleviated irritation of the eye. After administration of MT formulations to rabbit corneas, each harvested cornea was separated into corneal epithelium, stroma, and endothelium. MT concentrations in the corneal epithelium, stroma, and endothelium for the F1-treated group were 55.5±9.24, 26.7±2.66, and 21.1±1.77µM while those for the F2-treated group were 127.2±21.01, 43.7±16.93, and 51.0±13.91µM, respectively. Stability studies for 60days showed no significant change in pH, osmolarity, and MT content. In conclusion, MT/HPßCD formulations can lower irritation, enhance MT stability, and improve therapeutic efficacy.

Evaluation of tacrolimus sorption to PVC- and non-PVC-based tubes in administration sets: Pump method vs. drip method.

Tacrolimus sorption to tubes was evaluated using pump and drip methods For tubes, polyvinylchloride (PVC)- and non-PVC-based (polyurethane [PU] and polyolefin [PO]) tubes were used. First, inner surface properties of tubes were analyzed using field emission scanning electron microscopy and X-ray photoelectron spectroscopy. Tacrolimus was quantitatively analyzed using high-performance liquid chromatography with UV detection. For kinetic sorption analysis, diluted tacrolimus to 10µg/mL was passed through 1-m-long tubes at 10mL/h. Samples were collected at 1-4h. The inner surface of PO-based tubes was relatively smooth and soft compared with those of PVC- and PU-based tubes. Atomic compositions of tubes matched chemical formulas of polymers excluding low-level impurity in PVC-based tubes. Tacrolimus was successfully analyzed and linearly determined at 2.5-20µg/mL. From both methods, PVC- and PO-based tubes exhibited the highest and the lowest (<10%) sorption levels to tacrolimus, respectively. Tacrolimus was stably delivered using the pump method. Results suggested that the pump method can estimate tacrolimus sorption in administration set tubes and evaluate other sorptional drugs used at low concentrations. PO-based tubes also have promising potential as an alternative for administration set tubes.

Evaluation of Drug Sorption to PVC- and Non-PVC-based Tubes in Administration Sets Using a Pump.

Administration sets are delivery tools for the direct application of drugs into the body and are composed of a spike, a drip chamber, tubes, Luer adapters (connectors), a needle cover for protection, and other accessories. Drug sorption to tubes of administration sets is a critical issue in terms of safety and efficacy. Although drug sorption is an important factor in the quality of an administration set, there are no standard evaluation methods for the regulation of drug sorption to the tubes. Here, we describe an evaluation protocol for drug sorption to tubes of administration sets. Tubes made of polyvinyl chloride (PVC)- and non-PVC-based polymeric materials were cut to 1 m in length. Diazepam and tacrolimus were used as model drugs. In the kinetic sorption study, we selected the drug concentration and flow rate based on the clinical usage of these drugs. After the dilution of each drug in a glass bottle, the diluted drug solution was delivered through tubes of administration sets using a pump. Samples were collected in amber vials at appropriate time points and the drugs were analyzed using high-performance liquid chromatography. Drug concentrations and sorption levels to tubes of the administration sets were calculated. Acceptable criteria to ensure the quality of administration sets are recommended.

Gr-1intCD11b+ myeloid-derived suppressor cells accumulate in corneal allograft and improve corneal allograft survival.

We identified the characteristics of myeloid-derived suppressor cells (MDSCs) and investigated their mechanism of induction and their functional role in allograft rejection using a murine corneal allograft model. In mice, MDSCs coexpress CD11b and myeloid differentiation antigen Gr-1. Gr-1+CD11b+ cells infiltrated allografted corneas between 4 d and 4 wk after surgery; however, the frequencies of Gr-1+CD11b+ cells were not different between accepted and rejected allografts or in peripheral blood or BM. Of interest, Gr-1intCD11b+ cells, but not Gr-1hiCD11b+ cells, infiltrated the accepted graft early after surgery and expressed high levels of immunosuppressive cytokines, including IL-10, TGF-ß, and TNF-related apoptosis-inducing ligand. This population remained until 4 wk after surgery. In vitro, only high dose (>100 ng/ml) of IFN-γ plus GM-CSF could induce immunosuppressive cytokine expression in Gr-1intCD11b+ cells. Furthermore, adoptive transfer of Gr-1intCD11b+ cells reduced T cell infiltration, which improved graft survival. In conclusion, high-dose IFN-γ in allograft areas is essential for development of Gr-1intCD11b+ MDSCs in corneal allografts, and subtle environmental changes in the early period of the allograft can result in a large difference in graft survival.

Boiling Method-Based Zinc Oxide Nanorods for Enhancement of Adipose-Derived Stem Cell Proliferation.

Adipose-derived stem cells (ASCs) are typically expanded to acquire large numbers of cells for therapeutic applications. Diverse stimuli such as sphingosylphosphocholine and vitamin C have been used to increase the production yield and regenerative potential of ASCs. In the present study, we hypothesized that ZnO nanorods have promising potential for the enhancement of ASC proliferation. ZnO nanorods were prepared using three different methods: grinding and boiling at low temperature with and without surfactant. The physicochemical properties of the nanorods such as their crystallinity, morphology, size, and solvent compatibility were evaluated, and then, the ability of the synthesized ZnO nanorods to enhance ASC proliferation was investigated. Scanning electron microscopy images of all of the ZnO powders showed rod-shaped nanoflakes with lengths of 200-500 nm. Notably, although ZnO-G produced by the grinding method was well dispersed in ethanol, atomic force microscopy images of dispersions of both ZnO-B from boiling methods and ZnO-G indicated the presence of clusters of ZnO nanorods. In contrast, ZnO-B was freely dispersible in 5% dextrose of water and dimethyl sulfoxide, whereas ZnO-G and ZnO-M, produced by boiling with ethanolamine, were not. All three types of ZnO nanorods increased the proliferation of ASCs in a dose-dependent manner. These results collectively suggest that ZnO nanorods have promising potential for use as an agent for the enhancement of ASC proliferation.

Diazepam sorption to PVC- and non-PVC-based tubes in administration sets with quantitative determination using a high-performance liquid chromatographic method.

Diazepam is highly sorbed to the plastic materials of administration sets for intravenous infusion. This can be detrimental as it should be delivered to the patient at the administered amount for efficacy and safety. We report here the sorption levels of diazepam onto various types of tubes in administration sets. The tube materials of the administration sets included polyvinylchloride (PVC) and the non-PVC materials such as polyurethane (PU) and polyolefin (PO) were used. Two conditions of diazepam administered in preclinical and clinical settings were tested using an infusion pump. Injections were prepared by diluting diazepam to 20mg/500mL and 10mg/100mL in 5% dextrose. Diluted diazepam solutions at the concentrations of 10mg/100mL and 20mg/500mL were separately delivered through 1m of tubing at 1mL/min for 1.05 and 4.05h. Samples were analyzed using a high-performance liquid chromatography with UV detection. PVC- and PU-based tubes showed higher sorption of diazepam than did PO-based tubes. PO-based tubes delivered more than 90% of the administered diazepam. The results showed that PO-based tubes of administration sets have a promising potential to deliver hydrophobic drugs like diazepam with minimal sorption levels. In addition, the tube materials in administration sets may be one of the critical factors to ensure drug efficacy and safety.

Hair regeneration using adipose-derived stem cells.

Adipose-derived stem cells (ASCs) have been used in tissue repair and regeneration. Recently, it was reported that ASC transplantation promotes hair growth in animal experiments, and a conditioned medium of ASCs (ASC-CM) induced the proliferation of hair-compositing cells in vitro. However, ASCs and their conditioned medium have shown limited effectiveness in clinical settings. ASC preconditioning is one strategy that can be used to enhance the efficacy of ASCs and ASC-CM. Therefore, we highlighted the functional role of ASCs in hair cycle progression and also the advantages and disadvantages of their application in hair regeneration. In addition, we introduced novel ASC preconditioning methods to enhance hair regeneration using ASC stimulators, such as vitamin C, platelet-derived growth factor, hypoxia, and ultraviolet B.

Targeting L-type amino acid transporter 1 for anticancer therapy: clinical impact from diagnostics to therapeutics.

INTRODUCTION: L-type amino acid transporter 1 (LAT1) is one of the amino acid transporters. It is overexpressed in various types of cancer cells, while it is produced restrictedly in normal tissues. AREAS COVERED: We discuss its characteristics in cancer cells compared with normal cells. We also mention the current applications to target LAT1 for anticancer therapy focusing on prognostic biomarkers, radio-labeled tumor imaging reagents, amino acid-stapled prodrugs, LAT1-mediated enhanced transport of anticancer drugs and LAT1 inhibitors. EXPERT OPINION: LAT1 can be a versatile target to promisingly develop transporter-based drugs with enhanced drug delivery potential for anticancer therapy.

Comparative effects of PEG-containing liposomal formulations on in vivo pharmacokinetics of streptokinase.

Streptokinase (SK) is an effective thrombolytic agent, but it has a short half-life due to its rapid elimination from the body. In this study, we prepared and evaluated polyethyleneglycol (PEG)-based liposomal formulations (PEG-liposomes) containing SK with a view toward prolonging its circulatory half-life. SK-bearing liposomes (SK-liposomes) were prepared using freeze-thaw method after film hydration and extrusion techniques, composed of phosphatidylcholine [egg phosphatidylcholine (EPC), dipalmitoyl PC, or distearoyl PC], cholesterol and cholesterol-3-sulfate with or without PEG. Their physicochemical properties were characterized by the measurement of size and zeta potential and incorporation efficiency. SK-liposomal formulations were applied to rats through a femoral vein via intravenous administration to compare the effects of liposomal delivery and PEG on the half-life of SK in blood. Free SK was used as a control. SK activities in plasma were measured to estimate the amidolytic activity of SK-plasminogen complex after rupturing liposomes with Triton X-100. Pharmacokinetic parameters were obtained from SK activity-time profiles. The SK-liposomes had a homogenous distribution of negatively charged nanoparticles at the range of 10-33% of the incorporation efficiencies of SK. Among the SK-liposomes, SK-EPC- and SK-EPC/PEG-liposomes had injectable diameters (<200 nm). SK was administered as free SK, SK-EPC-liposomes, or SK-EPC/PEG-liposomes for in vivo study. SK-EPC/PEG-liposomes had significantly greater the t(1/2), AUC(∞) and MRT values of SK than SK alone or SK-EPC-liposomes. These findings suggest that PEG-liposomal incorporation of SK enhances thrombolytic activity in vivo, and that such liposomes can be utilized to enhance the pharmacokinetic profiles of other therapeutic proteins with a short biological half-life.

Dissolution and bioavailability of lercanidipine-hydroxypropylmethyl cellulose nanoparticles with surfactant.

The objective of this study was to develop lercanidipine-hydroxypropylmethyl cellulose (HPMC) nanoparticles with high oral bioavailability. The lercanidipine-HPMC nanoparticles with/without surfactants were manufactured using a supercritical antisolvent (SAS) process. Gelucire 44/14, poloxamer 407, and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were evaluated as surfactants. Spherical lercanidipine-HPMC nanoparticles with a mean particle size less than 400 nm were successfully prepared using a SAS process. The dissolution and oral bioavailability of lercanidipine was significantly increased by addition of surfactants. Especially lercanidipine-HPMC nanoparticles with TPGS showed a 2.47-fold higher oral bioavailability than raw material. Furthermore, the dissolution efficiency was strongly correlated to the in vivo Cmax and AUC0 → 24h. Therefore, the preparation of HPMC nanoparticles with TPGS using a SAS process is a highly effective formulation strategy for enhanced oral bioavailability of lercanidipine.