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The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients were selected. Self-emulsifying regions were identified by mixing the selected materials at various ratios, and a pseudoternary phase diagram was constructed by synthesizing these results. The various physicochemical properties of microemulsion incorporating olaparib were confirmed by investigating the morphology, particle size, zeta potential, drug content and stability. In addition, the improved dissolution and absorption of olaparib were also confirmed through a dissolution test and a pharmacokinetic study. An optimal microemulsion was generated in the formulation of Capmul® MCM 10%, Labrasol® 80% and PEG 400 10%. The fabricated microemulsions were well-dispersed in aqueous solutions, and it was also confirmed that they were maintained well without any problems of physical or chemical stability. The dissolution profiles of olaparib were significantly improved compared to the value of powder. Associated with the high dissolutions of olaparib, the pharmacokinetic parameters were also greatly improved. Taken together with the results mentioned above, the microemulsion could be an effective tool as a formulation for olaparib and other similar drugs.

The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble Olaparib. Through the solubility test of Olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients for use in SMEDDS manufacturing were selected. Self-emulsifying regions were identified by mixing the selected materials at various ratios, and a pseudoternary phase diagram was constructed by synthesizing these results. Various physicochemical properties of microemulsion incorporating Olaparib were confirmed by investigating the particle morphology, particle size, zeta potential, drug content and stability. In addition, the improved dissolution and oral absorption of Olaparib were also confirmed through a dissolution test and a pharmacokinetic study. An optimal microemulsion was generated in the formulation of Capmul MCM EP/NF 10%, Labrasol 80% and PEG 400 10%. Fabricated nano-sized microemulsions were well-dispersed in aqueous solutions, and it was also confirmed that it was maintained well without any problems of either physical or chemical stability. The 5 min initial dissolution of Olaparib in fabricated formulations was improved by 10.6 times (pH1.2), 14.8 times (pH6.8) and 14.8 times (distilled water) compared to the values of Olaparib powder. The dissolution at 120min was 45.4±4.0%(pH1.2), 53.5±1.1% (pH6.8) and 58.1±1.00% (distilled water) in Olaparib powder but has been significantly improved by 1.7 times (74.8±1.9%), 1.6 times (84.2±0.3%) and 1.5 times (81.2±0.7%) in SMEDDS. Associated with the high dissolutions of Olaparib in fabricated microemulsions, the pharmacokinetic parameters were also greatly improved. The Cmax and AUCinf of Olaparib in the prepared microemulsion were increased 4.2- and 3.2-fold, respectively, compared to powder. Taken together with the results mentioned above, the microemulsion system could be an effective tool as an oral delivery formulation for Olaparib. Additionally, our results demonstrate that the SMEDDS systems comprising Capmul MCM, Labrasol and PEG 400 could be a useful option for improvement of several other poorly water-soluble drugs with physico-chemical properties similar to Olaparib.

To develop an in vitro culture system for tissue engineering to mimic the in vivo environment and evaluate the applicability of ultrasound and PLGA particle system. For tissue engineering, large molecules such as growth factors for cell differentiation should be supplied in a controlled manner into the culture system, and the in vivo microenvironment need to be reproduced in the system for the regulation of cellular function. In this study, portable prototype ultrasound with low intensity was devised and tested for protein release from bovine serum albumin (BSA)-loaded poly(lactic-co-glycolic acid) (PLGA) particles. BSA-loaded PLGA particles were prepared using various types of PLGA reagents and their physicochemical properties were characterized including particle size, shape, or aqueous wetting profiles. The BSA-loaded formulation showed nano-ranged size distribution with optimal physical stability during storage period, and protein release behaviors in a controlled manner. Notably, the application of prototype ultrasound with low intensity influenced protein release patterns in the culture system containing the BSA-loaded PLGA formulation. The results revealed that the portable ultrasound set controlled by the computer could contribute for the protein delivery in the culture medium. This study suggests that combined application with ultrasound and protein-loaded PLGA encapsulation system could be utilized to improve culture system for tissue engineering or cell regeneration therapy.

The purpose of this study is to investigate the surface activity of starch nanocrystals (SNC), material derived from starch, and confirm their usefulness as a surfactant. In order to evaluate the surface activity, the surface tension change of suspended SNC solution via the Wilhelmy plate method was measured and the values were compared with various synthetic surfactants. The effect of SNC as emulsifier was evaluated on emulsion formation and physical stability. The surface tension of the SNC-dispersed solution was decreased while its concentration was increased. When the 5.0% (w/v) of SNC was added, the surface tension was decreased from 70.3 to 49.5 mN/m. It was confirmed that the physical stability of the emulsion prepared by adding the SNC was improved compared to that of surface inactivity material (PEG 400). The phase separation was observed within 1 hour after preparation of the emulsion containing PEG 400, but the emulsion containing SNC was stable for 5 hours or more. To summarize this study, SNC, a natural-derived and non-toxic material, exhibits sufficient surface activity, thereby confirming the possibility of being applied to the food and pharmaceutical industry.

Formation of an electrolyte complex using the electrostatic interactions between a polyanionic polymer and a cationic drug is a simple and efficient method of preparing a colloidal drug carrier system. Dextran sulfate, with a negatively charged sulfate group, was reacted in an acetate buffer solution of pH 3 with positively charged 1° amine, 2° amine, 3° amine, piperazine, and piperidine structures from 24 small-molecule drugs. The electrolyte complex was formed from 15 drugs, 63% of those tested. The tendency to form the electrolyte complex was in the order of piperazine and piperidine >3° amine >>2° amine. The drugs with the 1° amine structure failed to form an electrolyte complex. The mean particle sizes were in the range of 50-740 nm, and most of them showed a submicron colloidal dispersion of

Self-microemulsifying drug delivery systems represent a stable formulation for enhancing the solubility and absorption efficacy of poorly soluble drugs. In this study, a self-microemulsifying drug delivery system (SMEDDS) was designed and applied for oral administration of poorly water-soluble pazopanib, a Biopharmaceutical Classification Class II anticancer drug. The solubility of pazopanib was first evaluated using various oils, surfactants, and co-surfactants. Pseudoternary phase diagrams were plotted to identify the selfemulsifying region and the phase behavior of optimized vehicle selected after screening of oils, surfactants, and co-surfactants. The SMEDDS comprising Capmul MCM NF, Tween 80, and PEG 400 was fabricated for incorporating pazopanib. It exhibited spherical droplets with size of 86.9 ± 0.8 nm and zeta potential value of –14.7 ± 0.1 mV. In vitro dissolution profiles of the SMEDDS were 2.40-fold (pH 4.0) and 6.45-fold (pH 6.8) higher than that of pazopanib powder. In particular, pazopanib-SMEDDS showed pH-independent dissolution profiles. In vivo pharmacokinetic parameters of the SMEDDS revealed enhanced bioavailability of pazopanib, which was 3.32-fold higher than that of pazopanib powder when administered orally. Taken together, the SMEDDS is effective as an oral delivery vehicle for pazopanib. In addition, our findings demonstrate that self-microemulsifying drug delivery systems could be a potential tool for improving bioavailability of other poorly water-soluble drugs.

Over the last several decades, long-acting injections have been studied in order to overcome such problems as low bioavailability in the oral route, the short durations of action in conventional injection, and the poor medication adherence in patients. The authors classified long-acting injections into three categories, namely, molecular modification, nanovehicle carriers, and stimuli-responsive hydrogels. The mechanisms and practical cases of these long acting injectable formulations, including conventional and recent technologies, were described and discussed in this review. Long-acting injection formulations has been proven to be useful from a number of preclinical and clinical studies. Therefore, the long-acting injection technologies can be promising strategy for precision and personalized medicine if the characteristics of formulation such as extended release and the drug-targeting are used appropriately.

Recently, due to their promising applications in biomedicine, magnetic iron oxide nanoparticles (MPs) have become one of the research hotspots in the nanomedicine field. Since various synthetic modifications have been widely applied to these nanoparticles for better targeting behaviors, it is meaningful to apply the optimal magnetic field condition for each case. This will enable creating a safe and efficient drug targeting using different types of MPs. In the present study, we aimed to find out any changes of transepithelial transport of polysaccharide-coated MPs by applying the continuous or the pulsatile magnetic field condition. Our results with heparin-functionalized MPs indicate that the particle concentrations and the external magnetic field could influence the transepithelial permeability of the particles. In the presence of a continuously applied magnetic density, heparin-MPs at high concentrations, by forming magnetically-induced aggregation of particles over the cell surface layer, showed a lower cellular transport than those at low concentrations. Furthermore, the results from the quantitative chemical assays and imaging analyses showed that transepithelial transport of heparin-MPs (negatively charged) under the pulsatile magnetic field was higher than that under the continuous magnetic field (CP), whereas the starch-MPs (neutrally charged) showed a small difference in transepithelial transport or cell retention between pulsatile vs. continuous magnetic field conditions. Taken together, our results suggest that the external magnetic field should be differentially applied to control the cellular drug transport depending on the physicochemical properties of the surface chemistry of magnetic particles.

Ocular drug delivery has been a well-known route for the drug administration for the treatment of ocular diseases. However, numerous anatomical and physiological barriers prevailing in the eye itself create considerable challenges for achieving the necessitated therapeutic efficacy along with ocular bioavailability. However, recent advances in nanoengineered strategies hold definite promises in terms of devising improved ophthalmic medicines for the effective drug delivery to target the sites with enhanced ocular bioavailability. Curcumin, a hydrophobic polyphenol yellow colored compound, and its metabolic reduced product, tetrahydrocurcumin (THC), have been known for their beneficial pharmacological functions, such as anti-inflammatory or anti-oxidant activities at various tissue sites. However, the low aqueous solubility of these compounds results in their poor bioavailability, thereby limiting their widespread application. Therefore, in the present study, we investigated the changes in drug solubility by forming inclusion complexes with different derivatives of hydroxypropyl (HP)-cyclodextrins (CD). To this end, the spray drying technique was used for nanoengineering curcumin or THC-loaded formulations to improve the stability of formulations during the storage. The formulations were characterized in terms of physicochemical properties and cellular permeability. The results demonstrated that the encapsulation of curcumin (or THC) into the HP-CDs significantly increased the drug solubility and enhanced the corneal and retinal epithelial permeability. Curcumin or THC complexes in HP-CDs with improved bioavailability also induced anti-oxidant activity (SOD1, CAT1, and HMOX1) in higher levels in the ocular epithelial cells and showed oxidative protection effects in rabbit cornea tissues that will boost up their application in ocular medicine.

Ecabet has a mucosal protection and anti-Helicobacter pylori effect only by local action in the gastric mucous layer, due to an extremely poor absorption into the systemic blood circulation. The aim of the present work was to develop chitosan-ecabet electrolyte complex (ChE) for the enhanced mucosal drug delivery. ChEs were prepared with various ecabet-chitosan concentration ratios. Entrapment efficiency (%), sedimentation volume (%), transmission electron microscopy (TEM), FT-IR spectrum, and drug release were investigated. ChEs were prepared by the simple mixing method in a pH-adjusted solution based on the electrostatic interaction between the sulfonate (negatively charged) group from ecabet and the amine (positively charged) group from chitosan. Sedimentation volume and entrapment efficiency at the same concentration of ecabet sodium with that of chitosan resulted in 53.6% and 86.75%, respectively, suggesting a high degree of forming complex. In TEM images, the complex was approximately 200 nm in particle size and had loosely entangled particles. Forming complex of ChEs was supported by new bands appearance in the FT-IR spectrum. In the drug release study using dialysis membrane sac, ChEs showed a sustainable release up to 80% during 12 h as compared to ecabet sodium suspension at pH 1.2 medium. Based on the results of this work, ChE would be a promising drug delivery system for gastric mucosa.

The aim of this study is to develop nanosuspension for improved dissolution of poorly water-soluble celecoxib. We first prepared coarse suspension of celecoxib with Tween 80 and hydroxypropyl methylcellulose as stabilizers, and then fabricated nanosuspension using the bead milling technique. Depending on milling time, the physical properties of nanosuspension were evaluated by photon correlation spectroscopy (e.g., particle size and distribution) and scanning electron microscopy (SEM) (e.g., morphology). As results, the mean size of crystalline celecoxib particles was highly reduced (368.1±14.5 nm) as milling process proceeded comparing to celecoxib powder (6.5±1.0 μm). Morphology of milled celecoxib particles has changed considerably from bar-shape or plate-shape to needle-shape due to a high energy caused by milling. In the dissolution test, the celecoxib nanosuspension showed an improved dissolution profile at pH 1.2 compared to celecoxib powder (less than 1%). In contrast, 53.4% of celecoxib in nanosuspension was dissolved up to 30 minutes, demonstrating improved dissolution of celecoxib. Taken together, bead-milled nanosuspension could be an effective strategy that can improve the dissolution and bioavailability.

The aim of this work was to prepare and assess a self-nanoemulsifying drug delivery system (SNEDDS) containing water-insoluble orlistat that was used for the inhibition of lipase activity in gastrointestinal lumen. The pseudo-ternary phase diagram, composed of orlistat and medium chain triglycerides (MCT) as oil phase and Cremophor EL as surfactant, was made for the confirmation of giving SNEDDS preconcentrate. The physical state, particle size dispersed in water, dissolution and lipase inhibition of SNEDDS preconcentrates were investigated. The appointed SNEDDS preconcentrates in the pseudo-ternary phase diagram showed no endothermic peak of orlistat and a liquid state. The particle sizes of SNEDDS dispersed with water were uniform and in the range of

The aim of this study was to improve the skin accumulation of hydroxycitric acid by using ethosomes with nanosize. We fabricated nanosized ethosome for the topical delivery of hydrophilic hydroxycitric acid and evaluated their physical properties and furthermore cytotoxicity. As results, in cell-based experiments, the use of ethosomes encapsulating hydroxycitric acid extract reduced the lipid droplet deposition in differentiated adipocytes, which was visualized by Oil Red O staining assay and also quantitatively measured by a triglyceride assay. The observed reduction in lipid droplet deposition occurred in a hydroxycitric acid extract concentration-dependent manner. In addition, the high accumulation of hydroxycitric acid in murine skin (66.28%) was observed following treatment with hydroxycitric acid extract-loaded ethosomes compared with treatment with hydroxycitric acid alone (1.19%) without ethosome as a nanocarrier. Based on these results, our findings showed that nanosized ethosomes improved the topical delivery of hydroxycitric acid and thus reduced lipid droplet deposition in adipocytes.

Extracellular vesicles (EVs) are nanosized membrane particles secreted by cells to convey intercellular information. In recent years, EVs have enticed scientists owing to their prevalent distribution, enormous possibility as therapeutic aspirants, and probable roles as disease biomarkers. As natural transporters in the endogenous communication system, they play a role in protein, lipid, miRNA, mRNA, and DNA transport. In this chapter, we recapitulate the roles of EVs in the vast field of regenerative medicine. This summary mainly describes the potential roles of EVs in the regeneration of extensively studied organs or tissues, such as the heart, kidney, lung, liver, skin, and hair. Furthermore, EV can also transport drugs and corroborate their uptake by target cells through endocytosis; therefore, this chapter also highlights the use of EVs in the field of drug delivery.

The purpose of this study is to identify the effects of a stabilizer and matrix former in the development of a celecoxib dried nanosuspension (DNS) for high dissolution rate and drug loading. Tween 80 and Hydroxypropyl Methylcellulose (HPMC) were used as stabilizers in the bead-milling process and dextrin was used as the matrix former in the spray-drying. Various nanosuspensions (NS) were prepared by varying the ratio of HPMC and dextrin, and the physicochemical properties of each formulation were evaluated for particle size, morphology, drug loading, crystallinity, redispersibility, physical stability and dissolution rate. HPMC efficiently stabilized the NS system and reduced the particle size of NS. The mean particle size of the NS with 0.5% HPMC (w/v) was the smallest (248 nm) of all formulations. Dextrin has been shown to inhibit the increase of particle size efficiently, which is known to occur frequently when NS is being solidified. As the dextrin increased in DNS, the dissolution rates of reconstituted NS were significantly improved. However, it was confirmed that more than the necessary amount of dextrin in DNS reduced the dissolution and drug loading. The dissolution of celecoxib in DNS prepared at the ratio (drug:dextrin, 1:2.5) was almost the highest. The dissolution of optimal formulation was 95.8% at 120 min, which was 2.0-fold higher than that of NS dried without dextrin. In conclusion, these results suggest that the formulation based on Tween 80, HPMC and dextrin may be an effective option for DNS to enhance its in vitro dissolution and in vivo oral absorption.

Tenofovir disoproxil (TD) has narrow absorption site mostly in upper intestinal tract where tenofovir rapidly decomposes. The aim of this work was to prepare and evaluate tenofovir disoproxil-loaded enteric microparticles (TDEMs) for the enhanced duodenal delivery. TDEMs were composed of TD, eudragit L-100 (EL) and ethyl cellulose (EC) as release-controlling polymers. For the physicochemical characterization, TDEMs were evaluated in terms of encapsulation efficiency (EE%), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR). The dissolution test was also performed while continuously changing the medium pH. The EE% of TD in TDEMs was good and more than 90%. The EC and EL formed a physically mixed structure and maintained their respective properties in TDEMs as confirmed by SEM image and FT-IR analysis. Combination of EL and EC gave higher enteric properties to TDEMs than the single use of EL or EC. The optimized TDEM (TD/EL/EC = 0.2/1/1, w/w/w ratio) yielded mean dissolution rate less than 10% in 1 h at pH 1.2, but completed dissolution with a dissolution more than 85% within 1 h at pH 6.5. Thus, the suggested TDEM would be promising enteric microparticles for the intensive delivery of TD to the duodenum.

In this study, we aimed to develop a 20(S)-protopanaxadiol (PPD)-loaded self-nanoemulsifying drug delivery system (SNEDDS) preconcentrate (PSP) using comprehensive ternary phase diagrams for enhanced solubility, physical stability, dissolution, and bioavailability. Capmul MCM C8 and Capryol 90 were selected as the oil phase owing to the high solubility of PPD in these vehicles (&gt, 15%, w/w). Novel comprehensive ternary phase diagrams composed of selected oil, surfactant, and PPD were constructed, and the solubility of PPD and particle size of vehicle was indicated on them for the effective determination of PSP. PSPs were confirmed via particle size distribution, physical stability, and scanning electron microscope (SEM) with the dispersion of water. The optimized PSP (CAPRYOL90/Kolliphor EL/PPD = 54/36/10, weight%) obtained from the six possible comprehensive ternary phase diagrams showed a uniform nanoemulsion with the particle size of 125.07 &plusmn, 12.56 nm without any PPD precipitation. The PSP showed a dissolution rate of 94.69 &plusmn, 2.51% in 60 min at pH 1.2, whereas raw PPD showed negligible dissolution. In oral pharmacokinetic studies, the PSP group showed significantly higher Cmax and AUCinf values (by 1.94- and 1.81-fold, respectively) than the raw PPD group (p &lt, 0.05). In conclusion, the PSP formulation with outstanding solubilization, dissolution, and in-vivo oral bioavailability could be suggested using effective and comprehensive ternary phase diagrams.

Extracellular vesicles (EVs) are nanosized membrane particles secreted by cells to convey intercellular information. In recent years, EVs have enticed scientists owing to their prevalent distribution, enormous possibility as therapeutic aspirants, and probable roles as disease biomarkers. As natural transporters in the endogenous communication system, they play a role in protein, lipid, miRNA, mRNA, and DNA transport. In this chapter, we recapitulate the roles of EVs in the vast field of regenerative medicine. This summary mainly describes the potential roles of EVs in the regeneration of extensively studied organs or tissues, such as the heart, kidney, lung, liver, skin, and hair. Furthermore, EV can also transport drugs and corroborate their uptake by target cells through endocytosis; therefore, this chapter also highlights the use of EVs in the field of drug delivery.

Cenobamate is a candidate drug that is being evaluated in a phase 3 clinical trial as an epilepsy treatment. In the present study, we developed and validated a liquid chromatography-tandem mass spe...

Dae Hun Kim,1,* Jae Yeol Kim,1,* Rae Man Kim,1 Pooja Maharjan,1 Yu-Geun Ji,2 Dong-Jin Jang,3 Kyoung Ah Min,1 Tae-Sung Koo,2 Kwan Hyung Cho1 1Department of Pharmacy, Inje Institute of Pharmaceutical Sciences and Research, Inje University, Gimhae, Republic of Korea; 2Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon, Republic of Korea; 3Department of Pharmaceutical Engineering, Inje University, Gimhae, Republic of Korea *These authors contributed equally to this work Background: The present study aimed to develop orlistat-loaded solid self-nanoemulsifying drug delivery system preconcentrate (SSP) with the minimum use of lipid excipients for the enhanced solubility, in vitro dissolution, lipase inhibition, and in vivo performance. Materials and methods: In the screening of solubilizing vehicles, Solutol HS15 and Lauroglycol 90 were selected as the surfactant and oil phase, respectively. A pseudo-ternary phase diagram composed of Solutol HS15, Lauroglycol 90, and orlistat as an anti-obesity agent and lipid component was constructed, and the SSP regions were confirmed in terms of the particle size distribution in water, melting point by differential scanning calorimetry, and crystallinity by X-ray diffraction. Results: Physicochemical interaction between Solutol HS15 and orlistat resulted in SSP with various melting points in the range of 26°C~33°C. The representative maximum orlistat-loaded SSP (orlistat/Solutol HS15/Lauroglycol 90=55/40/5, weight ratio) showed the melting point of 32.23°C and constructed uniform nanoemulsion with the particle size of 141.7±1.1 nm dispersed in water. In the dissolution test at pH 1.2 without any detergent, the SSP reached 98.12%±0.83% until 45 minutes, whereas raw orlistat showed no significant dissolution rate. The dissolution samples containing SSP showed a lipase inhibition of 90.42%±1.58% within 45 minutes. In terms of the reduction level of fat absorption in rats, the intake group of SSP gave a significantly higher fat excretion into stool than the one observed in the raw orlistat group (P

Ocular drug delivery has been widely recognized as an attractive route for drug administration for cures of ocular diseases. Overall, designing an effective therapy to cure ocular diseases has been considered as a formidable task. Even though some infectious or inflammatory eye diseases could be alleviated by eye drops or ointments, achieving the required therapeutic efficacy along with ocular bioavailability remains a challenge due to the numerous anatomical and physiological barriers prevailing in the eye. Drug delivery to the posterior segment of the eye is yet a more challenging task. In this context, a better understanding of physiologic natures of the eyes and ocular pharmacokinetics would facilitate the development of new drug delivery systems to treat various vision-threatening disorders. For the effective drug delivery to target sites and to enhance the ocular bioavailability, recent progress in formulation strategies using nanotechnologies holds promises in terms of devising improved ophthalmic medicines. Hence, this review presents an overview of various aspects of ocular drug delivery, with a specific emphasis on nanocarrier-based strategies, including physiological barriers in eyes and conventional drug formulations. Recent research on sustained, controlled, and targeted systems for ocular drug delivery was updated as well.

The purpose of this study was to develop and evaluate a dry elixir (DE) system for enhancing the dissolution rate and oral bioavailability of celecoxib. DE system has been used for improving solubility, oral bioavailability of poorly water-soluble drugs. The encapsulated drugs or solubilized drugs in the matrix are rapidly dissolved due to the co-solvent effect, resting in both an enhanced dissolution and bioavailability. DEs containing celecoxib were prepared by spray-drying method and characterized by morphology, drug/ethanol content, drug crystallinity, dissolution rate and oral bioavailability. The ethanol content and drug content in DE system could be easily altered by controlling the spraydrying conditions. The dissolution profile of celecoxib from DE proved to be much higher than that of celecoxib powder due to the nano-structured matrix, amorphous state and encapsulated ethanol. The bioavailability of celecoxib from DEs was compared with celecoxib powder alone and commercial product (Celebrex®) in rats. In particular, blood concentrations of celecoxib form DE formulation were much greater than those of native celecoxib and market product. The data demonstrate that the DE system could provide an useful solid dosage form to enhance the solubility, dissolution rate and oral bioavailability of celecoxib.

Cancer immunotherapy orchestrates the immune system of the human body to fight against cancer cells. By doing this, it has revolutionized cancer treatment. Toxicities arising from dose-limit and low rates of patient response continue to be the major bottlenecks in clinical outcomes. The immune system has a close relationship with tumor. This leads to the combination of nanotechnology and immunotherapy. Nanotechnology can potentiate the efficacy of immunotherapy by enhancing the delivery and retention, and narrowing the toxicity of immunomodulation. In this regard, immunotherapy can combine with nanomedicine to give strategies that could lessen the side effects and improve clinical outcomes in patient populations. In this review, we explore and recapitulate recent advances in nanoparticle-based cancer immunotherapy.

Mistletoes, hemiparasites, contain many components with various biological activities and have been used in cosmetics industry. Loranthacease (1,000 species) and Viscaceae (550 species) have the most dominant species in mistletoes (nearly 1,600 species). It can be expected that the biological activities vary from species to species; therefore, we have tested

The purpose of this study is to develop a solid dispersion system with improved dissolution, absorption, and patient compliance of poorly water-soluble celecoxib (CXB). Instead of sodium lauryl sulfate (SLS), an anionic surfactant used in the marketed product (Celebrex&reg, ), solubilization was performed using non-ionic surfactants with low toxicity. Cremophor RH40 (Cre-RH) was selected as the optimal solubilizer. Granules and tablets containing CXB and Cre-RH were prepared via fluid-bed and tableting processes, respectively. The morphology, crystallinity, flowability, dissolution, and pharmacokinetics for CXB-solid dispersion granules (SDGs) and the hardness and friability for CXB-solid dispersion tablets (SDTs) were evaluated. The solubility of CXB was found to be increased by about 717-fold when using Cre-RH. The dissolution of granules containing Cre-RH was found to be increased greatly compared with CXB API and Celebrex&reg, (66.9% versus 2.3% and 37.2% at 120 min). The improvement of the dissolution was confirmed to be the same as that of granules in tablets. The CXB formulation resulted in 4.6- and 4.9-fold higher AUCinf and Cmax of CXB compared with those of an oral dose of CXB powder in rats. In short, these data suggest that the solid dispersion based on Cre-RH&mdash, a non-toxic solubilizer, non-ionic surfactant&mdash, may be an effective formulation for CXB to enhance its oral bioavailability and safety.

We have developed liposomes modified with various surface-charged lipids in order to solubilize the new algicidal agent, N-[(3,4-dichlorophenyl)methyl]cyclohexanamine (DP92), and enhance its algicidal activity against harmful algal blooms (HABs). The effect of liposome surface charge on algicidal activity was evaluated by using positively charged and neutral liposomes. The algicidal activity of the developed liposomes was evaluated by monitoring the inhibition of the growth rates of HABs (Heterosigma circularisquama (HC) and Heterosigma akashiwo (HA)). The algicidal activity of the liposomes was 2–6 times stronger compared to that of control. The solubilization of DP92 by entrapment in liposomes increased the solubility of DP92 and improved its algicidal activity up to sixfold. The electrostatic interaction between the negatively charged cell walls of HABs and the cationic liposomes additionally enhanced the algicidal activity of DP92.