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1.
Nanomaterials (Basel) ; 14(7)2024 Mar 28.
Article in English | MEDLINE | ID: mdl-38607132

ABSTRACT

Wind energy holds potential for in-situ powering large-scale distributed wireless sensor nodes (WSNs) in the Internet of Things (IoT) era. To achieve high performance in wind energy harvesting, a coaxial counter-rotating triboelectric nanogenerator with lift-drag hybrid blades, termed CCR-TENG, has been proposed. The CCR-TENG, which can work in non-contact and soft-contact modes, realizes low-speed wind energy harvesting through a combination of counter-clockwise rotating lift-type blades and clockwise rotating drag-type blades. Non-contact CCR-TENG realizes low-speed wind energy harvesting at wind speeds as low as 1 m/s. The output of a CCR-TENG, working in soft-contact mode, achieves 41% promotion with a maximum short-circuit current of 0.11 mA and a peak surface power density of 6.2 W/m2 with two TENGs connected in parallel. Furthermore, the power density per unit of wind speed achieves 746 mW/m3·s/m. Consequently, two fluorescent lamps were successfully illuminated and six temperature sensors were continuously lit by the CCR-TENG. The reported CCR-TENG significantly improves low-speed environmental wind energy utilization and demonstrates broad application prospects for in-situ power supply of distributed wireless transmission devices and sensors in the era of the IoT.

2.
Small ; 20(15): e2307680, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38012528

ABSTRACT

Self-powered vibration sensor is highly desired for distributed and continuous monitoring requirements of Industry 4.0. Herein, a flexible fiber-shaped triboelectric nanogenerator (F-TENG) with a coaxial core-shell structure is proposed for the vibration monitoring. The F-TENG exhibits higher adaptability to the complex surfaces, which has an outstanding application prospect due to vital compensation for the existing rigid sensors. Initially, the contact characteristics between the dielectric layers, that related to the perceiving performance of the TENG, are theoretically analyzed. Such a TENG with 1D structure endows high sensitivity, allowing for accurately responding to a wide range of vibration frequencies (0.1 to 100 Hz). Even applying to the real diesel engine, the error in detecting the vibration frequencies is only 0.32% compared with the commercial vibration sensor, highlighting its potential in practical application. Further, assisted by deep learning, the recognition accuracy in monitoring nine operating conditions of the system achieves 97.87%. Overall, the newly designed F-TENG with the merits of high-adaptability, cost-efficiency, and self-powered, has offered a promising solution to fulfill an extensive range of vibration sensing applications in the future.

3.
Small ; : e2308491, 2023 Dec 06.
Article in English | MEDLINE | ID: mdl-38054766

ABSTRACT

Developing desirable sensors is crucial for underwater perceptions and operations. The perceiving organs of marine creatures have greatly evolved to react accurately and promptly underwater. Inspired by the fish lateral line, this study proposes a triboelectric dynamic pressure sensor for underwater perception. The biomimetic lateral line sensor (BLLS) has high sensitivity to the disturbance amplitude/frequency, good adaptability to underwater environments and (relative) low cost. The sensors are deployed at the bottom of the test basin to perceive various moving objects, such as a robotic fish, robotic seal, etc. By analyzing the electrical signal of the sensor, the motion parameters of the objects passed over can be obtained. By monitoring signal variations across multiple sensors, the ability to sense different disturbance movement trajectories, including linear and angular trajectories, is achievable. The study will prove significant in forming an unconventional underwater perceiving method, which can back-up the sonic/optical sensors when are impaired in complex underwater environments.

4.
Pharmaceutics ; 15(12)2023 Dec 15.
Article in English | MEDLINE | ID: mdl-38140125

ABSTRACT

The nano-delivery system with a dual biomimetic effect can penetrate deeper in tumor microenvironments (TMEs) and release sufficient antitumor drugs, which has attracted much attention. In this study, we synthesized erythrocyte-like mesoporous silica nanoparticles (EMSNs) as the core loaded with doxorubicin (DOX) and coated them with calcium phosphate (CaP) and erythrocyte membrane (EM) to obtain DOX/EsPMs. The transmission electron microscopy (TEM), fluorescent co-localization and protein bands of SDS-PAGE were used to confirm the complete fabrication of EsPMs. The EsPMs with erythrocyte-like shape exhibited superior penetration ability in in vitro diffusion and tumor-sphere penetration experiments. Intracellular Ca2+ and ROS detection experiments showed that the CaP membranes of EsPMs with pH-sensitivity could provide Ca2+ continuously to induce reactive oxide species' (ROS) generation in the TME. The EM as a perfect "camouflaged clothing" which could confuse macrophagocytes into prolonging blood circulation. Hemolysis and non-specific protein adsorption tests proved the desirable biocompatibility of EsPMs. An in vivo pharmacodynamics evaluation showed that the DOX/EsPMs group had a satisfactory tumor-inhibition effect. These advantages of the nano-erythrocytes suggest that by modifying the existing materials to construct a nano-delivery system, nanoparticles will achieve a biomimetic effect from both their structure and function with a facilitated and sufficient drug release profile, which is of great significance for antitumor therapy.

5.
Nanomaterials (Basel) ; 13(10)2023 May 19.
Article in English | MEDLINE | ID: mdl-37242092

ABSTRACT

Sound wave is an extensively existing mechanical wave, especially in marine and industrial plants where low-frequency acoustic waves are ubiquitous. The effective collection and utilization of sound waves provide a fresh new approach to supply power for the distributed nodes of the rapidly developing Internet of Things technology. In this paper, a novel acoustic triboelectric nanogenerator (QWR-TENG) was proposed for efficient low-frequency acoustic energy harvesting. QWR-TENG consisted of a quarter-wavelength resonant tube, a uniformly perforated aluminum film, an FEP membrane, and a conductive carbon nanotube coating. Simulation and experimental studies showed that QWR-TENG has two resonance peaks in the low-frequency range, which effectively extends the response bandwidth of acoustic-electrical conversion. The structural optimized QWR-TENG has excellent electrical output performance, and the maximum output voltage, short-circuit current and transferred charge are 255 V, 67 µA, and 153 nC, respectively, under the acoustic frequency of 90 Hz and sound pressure level of 100 dB. On this basis, a conical energy concentrator was introduced to the entrance of the acoustic tube, and a composite quarter-wavelength resonator-based triboelectric nanogenerator (CQWR-TENG) was designed to further enhance the electrical output. Results showed that the maximum output power and the power density per unit pressure of CQWR-TENG reached 13.47 mW and 2.27 WPa-1m-2, respectively. Application demonstrations indicated that QWR/CQWR-TENG has good capacitor charging performance and is expected to realize power supply for distributed sensor nodes and other small electrical devices.

6.
Pharmaceutics ; 15(4)2023 Apr 03.
Article in English | MEDLINE | ID: mdl-37111615

ABSTRACT

In this study, we synthesized hollow mesoporous silica nanoparticles (HMSNs) coated with polydopamine (PDA) and a D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS)-modified hybrid lipid membrane (denoted as HMSNs-PDA@liposome-TPGS) to load doxorubicin (DOX), which achieved the integration of chemotherapy and photothermal therapy (PTT). Dynamic light scattering (DLS), transmission electron microscopy (TEM), N2 adsorption/desorption, Fourier transform infrared spectrometry (FT-IR), and small-angle X-ray scattering (SAXS) were used to show the successful fabrication of the nanocarrier. Simultaneously, in vitro drug release experiments showed the pH/NIR-laser-triggered DOX release profiles, which could enhance the synergistic therapeutic anticancer effect. Hemolysis tests, non-specific protein adsorption tests, and in vivo pharmacokinetics studies exhibited that the HMSNs-PDA@liposome-TPGS had a prolonged blood circulation time and greater hemocompatibility compared with HMSNs-PDA. Cellular uptake experiments demonstrated that HMSNs-PDA@liposome-TPGS had a high cellular uptake efficiency. In vitro and in vivo antitumor efficiency evaluations showed that the HMSNs-PDA@liposome-TPGS + NIR group had a desirable inhibitory activity on tumor growth. In conclusion, HMSNs-PDA@liposome-TPGS successfully achieved the synergistic combination of chemotherapy and photothermal therapy, and is expected to become one of the candidates for the combination of photothermal therapy and chemotherapy antitumor strategies.

7.
Small ; 19(22): e2300401, 2023 Jun.
Article in English | MEDLINE | ID: mdl-36840670

ABSTRACT

With the development of autonomous/smart technologies and the Internet of Things (IoT), tremendous wireless sensor nodes (WSNs) are of great importance to realize intelligent mechanical engineering, which is significant in the industrial and social fields. However, current power supply methods, cable and battery for instance, face challenges such as layout difficulties, high cost, short life, and environmental pollution. Meanwhile, vibration is ubiquitous in machinery, vehicles, structures, etc., but has been regarded as an unwanted by-product and wasted in most cases. Therefore, it is crucial to harvest mechanical vibration energy to achieve in situ power supply for these WSNs. As a recent energy conversion technology, triboelectric nanogenerator (TENG) is particularly good at harvesting such broadband, weak, and irregular mechanical energy, which provides a feasible scheme for the power supply of WSNs. In this review, recent achievements of mechanical vibration energy harvesting (VEH) related to mechanical engineering based on TENG are systematically reviewed from the perspective of contact-separation (C-S) and freestanding modes. Finally, existing challenges and forthcoming development orientation of the VEH based on TENG are discussed in depth, which will be conducive to the future development of intelligent mechanical engineering in the era of IoT.

8.
Materials (Basel) ; 15(10)2022 May 21.
Article in English | MEDLINE | ID: mdl-35629721

ABSTRACT

Pervasive and continuous energy solutions are highly desired in the era of the Internet of Things for powering wide-range distributed devices/sensors. Wind energy has been widely regarded as an ideal energy source for distributed devices/sensors due to the advantages of being sustainable and renewable. Herein, we propose a high-performance flag-type triboelectric nanogenerator (HF-TENG) to efficiently harvest widely distributed and highly available wind energy. The HF-TENG is composed of one piece of polytetrafluoroethylene (PTFE) membrane and two carbon-coated polyethylene terephthalate (PET) membranes with their edges sealed up. Two ingenious internal-structure designs significantly improve the output performance. One is to place the supporting sponge strips between the PTFE and the carbon electrodes, and the other is to divide the PTFE into multiple pieces to obtain a multi-degree of freedom. Both methods can improve the degree of contact and separation between the two triboelectric materials while working. When the pair number of supporting sponge strips is two and the degree of freedom is five, the maximum voltage and current of HF-TENG can reach 78 V and 7.5 µA, respectively, which are both four times that of the untreated flag-type TENG. Additionally, the HF-TENG was demonstrated to power the LEDs, capacitors, and temperature sensors. The reported HF-TENG significantly promotes the utilization of the ambient wind energy and sheds some light on providing a pervasive and sustainable energy solution to the distributed devices/sensors in the era of the Internet of Things.

9.
Colloids Surf B Biointerfaces ; 212: 112357, 2022 Apr.
Article in English | MEDLINE | ID: mdl-35101825

ABSTRACT

As is well known to all, delivering drug precisely to the tumor site is beneficial to improve antitumor effect. In this study, we reported mesoporous silica nanoparticles (MSNs) coated with dual-film of calcium carbonate (CaCO3) and lipid bilayer (denoted as MSNs@CaCO3@liposomes) innovatively which achieve sustained drug release anchored at tumor microenvironment and enhanced biocompatibility. The pH-sensitive CaCO3 film acted as a guide to cap the pore channels of MSNs allowed pH-triggered drug release when transporting into cancer cells. Furthermore, MSNs@CaCO3 was capsuled by lipid bilayer to improve cellular uptake efficiency and biocompatibility in blood circulation. Morphology of nanoparticles was characterized by transmission electron microscopy (TEM) and field emission scanning electron microscopy (FESEM) to confirm that double films were coated successfully. Doxorubicin hydrochloride (DOX) was efficaciously loaded into mesoporous pores as a model drug with a high drug loading content of 28%, forming DOX-loaded MSNs@CaCO3@liposomes (DOX/MSNs@CaCO3@liposomes). Non-specific protein adsorption and hemolysis test revealed enhanced biocompatibility. Drug release study in vitro showed DOX/MSNs@CaCO3@liposomes could delay to release DOX at pH 5.0 and avoid releasing at pH 7.4. In vitro and in vivo antitumor efficiency evaluation showed that DOX/MSNs@CaCO3@liposomes have a desirable inhibitory activity on tumor growth. Therefore, dual-film coated MSNs could be a good candidate for an antitumor drug delivery system.


Subject(s)
Nanoparticles , Silicon Dioxide , Calcium Carbonate , Doxorubicin/chemistry , Doxorubicin/pharmacology , Drug Carriers/chemistry , Drug Delivery Systems , Drug Liberation , Hydrogen-Ion Concentration , Liposomes , Nanoparticles/chemistry , Porosity , Silicon Dioxide/chemistry
10.
J Control Release ; 342: 1-13, 2022 02.
Article in English | MEDLINE | ID: mdl-34864116

ABSTRACT

The efficacy of oral insulin drug delivery is seriously hampered by multiple gastrointestinal barriers, especially transepithelial barriers, including apical endocytosis, lysosomal degradation, cytosolic diffusion and basolateral exocytosis. In this study, a functional nanoparticle (PG-FAPEP) with dual-modification was constructed to sequentially address these important absorption obstacles for improved oral insulin delivery. The dual surface decorations folate and charge-convertible tripeptide endowed PG-FAPEP with the ability to target the apical and basolateral sides of enterocytes, respectively. After fast diffusion across the mucus layer, PG-FAPEP could be efficiently internalized into epithelial cells via a folate receptor-mediated pathway and subsequently became positively charged in acidic lysosomes due to the surface tripeptide, triggering the proton sponge effect to escape lysosomes. When entering the cytosolic medium, PG-FAPEP was converted to neutral charge again, attenuating intracellular adhesion, and gained improved motility toward the basolateral side. Finally, the tripeptide helped PG-FAPEP recognize the proton-coupled oligopeptide transporter (PHT1) in the basolateral membrane, boosting intact exocytosis across intestinal epithelial cells. The in vivo studies further verified that PG-FAPEP could traverse the intestinal epithelium by folate receptor-mediated endocytosis, lysosomal escape, and PHT1-mediated exocytosis, exhibiting a high oral insulin bioavailability of 14.3% and a prolonged hypoglycemic effect. This formulation addresses multiple absorption barriers on demand with a simple dual-modification strategy. Therefore, these features allow PG-FAPEP to unleash the potential of oral macromolecule delivery.


Subject(s)
Insulin , Nanoparticles , Administration, Oral , Caco-2 Cells , Drug Carriers/chemistry , Drug Delivery Systems , Humans , Intestinal Absorption , Nanoparticles/chemistry
11.
Nanomaterials (Basel) ; 11(12)2021 Dec 17.
Article in English | MEDLINE | ID: mdl-34947780

ABSTRACT

Harvesting acoustic energy in the environment and converting it into electricity can provide essential ideas for self-powering the widely distributed sensor devices in the age of the Internet of Things. In this study, we propose a low-cost, easily fabricated and high-performance coniform Helmholtz resonator-based Triboelectric Nanogenerator (CHR-TENG) with the purpose of acoustic energy harvesting. Output performances of the CHR-TENG with varied geometrical sizes were systematically investigated under different acoustic energy conditions. Remarkably, the CHR-TENG could achieve a 58.2% higher power density per unit of sound pressure of acoustic energy harvesting compared with the ever-reported best result. In addition, the reported CHR-TENG was demonstrated by charging a 1000 µF capacitor up to 3 V in 165 s, powering a sensor for continuous temperature and humidity monitoring and lighting up as many as five 0.5 W commercial LED bulbs for acoustic energy harvesting. With a collection features of high output performance, lightweight, wide frequency response band and environmental friendliness, the cleverly designed CHR-TENG represents a practicable acoustic energy harvesting approach for powering sensor devices in the age of the Internet of Things.

12.
Int J Pharm ; 608: 121059, 2021 Oct 25.
Article in English | MEDLINE | ID: mdl-34474115

ABSTRACT

Ascorbic palmitate (AP) is widely used in the topical pharmaceutical or cosmetic formulations for melasma treatment. However, the presence of the skin barriers makes it difficult for the highly lipophilic drug molecules to traverse the stratum corneum (SC) and diffuse into the viable epidermis (EP) to reach the melanocytes, thereby exerting suboptimal antimelasma effects. Herein, AP was encapsulated into the transfersomes (TFs), yielding AP-TFs. AP-TFs utilized the deformability of TFs to squeeze through the skin pores in the SC under the transepidermal hydration gradient forces, leading to 14.1-fold increase in AP accumulation to the EP. AP-TFs could slowly release the encapsulated AP, while whether the released AP or transfersomal AP showed comparable uptake into the melanocytes, thereby exerting similar inhibitory effects on tyrosinase activity and melanogenesis. Ultimately, in the rat melasma model, AP-TFs showed superior antimelasma efficacy to free AP, with effective relief of oxidative stress and inflammation in the skin. Moreover, AP-TFs did not induce skin irritation. Therefore, the study provides a safe and effective approach to elevating the delivery of highly lipophilic drugs to the EP for enhanced treatment of melasma.


Subject(s)
Melanosis , Palmitates , Animals , Epidermis , Melanocytes , Melanosis/drug therapy , Rats , Skin
13.
Eur J Pharm Biopharm ; 169: 1-11, 2021 Dec.
Article in English | MEDLINE | ID: mdl-34461213

ABSTRACT

Abundant existence of extracellular matrix biological hydrogels in solid tumors precludes most therapeutics to arrive at intracellular target sites, which is probably one of the threatened reasons of pancreatic ductal adenocarcinoma (PDAC) for public health. In this study, we designed a rod-shaped protocell nanoparticle loading with doxorubicin hydrochloride (Dox) and indocyanine green (ICG), denoted as Dox/ICG-RsPNs, for enhanced chemo-photothermal PDAC treatment. The enhanced therapeutic efficacy was achieved by successively enhancing penetration across matrix hydrogels, endocytosis, increasing local temperature under laser irradiation and hyperthermia-triggered Dox release to nucleus. We found that RsPNs with rod shape could easily penetrate across matrix hydrogel, exerting excellent tumor accumulation. Then RsPNs was internalized effectively by BxPC-3 cells via a caveolin-mediated endocytosis pathway. In addition, ICG endowed the Dox/ICG-RsPNs with photothermal effect and the photothermal conversion efficiency was calculated for 16.2%. Under irradiation, a great number of Dox transported to the nucleus via hyperthermia-induced release. Furthermore, we found that the relative tumor volume of Dox/ICG-RsPNs was merely 1.37 under irradiation at the end of pharmacodynamic studies, which was significantly lower than that of other groups. These findings will provide a promise on the rational design of drug delivery system for effective chemo-photothermal combination therapy to treat PDAC.


Subject(s)
Doxorubicin/pharmacology , Drug Therapy/methods , Hyperthermia, Induced/methods , Indocyanine Green/pharmacology , Photothermal Therapy/methods , Animals , Antibiotics, Antineoplastic/pharmacology , Artificial Cells , Biological Availability , Cell Line, Tumor , Coloring Agents/pharmacology , Extracellular Matrix , Humans , Mice , Nanoparticle Drug Delivery System/pharmacology , Pancreatic Neoplasms , Treatment Outcome , Pancreatic Neoplasms
14.
Pharmaceutics ; 12(2)2020 Feb 10.
Article in English | MEDLINE | ID: mdl-32050600

ABSTRACT

This work explored absorption efficacy via an in vivo imaging system and parallel artificial membrane penetration in indomethacin (IMC) solid dispersion (SD) systems. Two different polymer excipients-hydroxypropyl methylcellulose (HPMC) and Kollicoat IR as precipitation inhibitors (PIs)-combined with mesoporous silica nanoparticles (MSNs) as carriers were investigated. The IMC-SDs were prepared using the solvent evaporation method and characterized by solubility analysis, infrared (IR) spectroscopy, powder X-ray diffraction (PXRD), field emission scanning electron microscopy (FESEM), and differential scanning calorimetry (DSC). It was confirmed that IMC successfully changed into an amorphous state after loading into the designed carriers. The in vitro release and stability experiments were conducted to examine the in vitro dissolution rates of IMC-SDs combined with HPMC and Kollicoat IR as PIs which both improved approximately three-fold to that of the pure drug. Finally, in vivo studies and in vitro parallel artificial membrane penetration (PAMPA) experiments ensured the greater ability of enhancing the dissolution rates of pure IMC in the gastrointestinal tract by oral delivery. In brief, this study highlights the prominent role of HPMC and Kollicoat IR as PIs in MSN SD systems in improving the bioavailability and gastrointestinal oral absorption efficiency of indomethacin.

15.
Nano Lett ; 20(2): 936-946, 2020 02 12.
Article in English | MEDLINE | ID: mdl-31671946

ABSTRACT

Despite rapid advancements in antitumor drug delivery, insufficient intracellular transport and subcellular drug accumulation are still issues to be addressed. Cancer cell membrane (CCM)-camouflaged nanoparticles (NPs) have shown promising potential in tumor therapy due to their immune escape and homotypic binding capacities. However, their efficacy is still limited due to inefficient tumor penetration and compromised intracellular transportation. Herein, a yolk-shell NP with a mesoporous silica nanoparticle (MSN)-supported PEGylated liposome yolk and CCM coating, CCM@LM, was developed for chemotherapy and exhibited a homologous tumor-targeting effect. The yolk-shell structure endowed CCM@LM with moderate rigidity, which might contribute to the frequent transformation into an ellipsoidal shape during infiltration, leading to facilitated penetration throughout multicellular spheroids in vitro (up to a 23.3-fold increase compared to the penetration of membrane vesicles). CCM@LM also exhibited a cellular invasion profile mimicking an enveloped virus invasion profile. CCM@LM was directly internalized by membrane fusion, and the PEGylated yolk (LM) was subsequently released into the cytosol, indicating the execution of an internalization pathway similar to that of an enveloped virus. The incoming PEGylated LM further underwent efficient trafficking throughout the cytoskeletal filament network, leading to enhanced perinuclear aggregation. Ultimately, CCM@LM, which co-encapsulated low-dose doxorubicin and the poly(ADP-ribose) polymerase inhibitor, mefuparib hydrochloride, exhibited a significantly stronger antitumor effect than the first-line chemotherapeutic drug Doxil. Our findings highlight that NPs that can undergo facilitated tumor penetration and robust intracellular trafficking have a promising future in cancer chemotherapy.


Subject(s)
Antineoplastic Agents/pharmacology , Drug Delivery Systems , Nanoparticles/chemistry , Neoplasms/drug therapy , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Membrane/chemistry , Coated Vesicles/chemistry , Doxorubicin/analogs & derivatives , Doxorubicin/chemistry , Doxorubicin/pharmacology , Humans , Polyethylene Glycols/chemistry , Polyethylene Glycols/pharmacology , Silicon Dioxide/chemistry , Spheroids, Cellular/chemistry
16.
ACS Appl Mater Interfaces ; 11(50): 46614-46625, 2019 Dec 18.
Article in English | MEDLINE | ID: mdl-31747243

ABSTRACT

Cell membrane-coated nanocarriers have been developed for drug delivery due to their enhanced blood circulation and tissue targeting capacities; however, previous works have generally focused on spherical nanoparticles and extracellular barriers. Many living organisms with different shapes, such as rod-shaped bacilli and rhabdovirus, display different functionalities regarding tissue penetration, cellular uptake, and intracellular distribution. Herein, we developed cancer cell membrane (CCM)-coated nanoparticles with spherical and rod shapes. CCM-coated nanorods (CRs) showed superior endocytosis efficiency compared with their spherical counterparts (CCM-coated nanospheres, CSs) due to the caveolin-mediated pathway. Moreover, CRs can effectively accumulate in the endoplasmic reticulum (ER) region and ship the loaded DOX to the nucleus at a considerable concentration, resulting in ER stress and subsequent apoptosis. After intravenous injection into human pancreatic adenocarcinoma cell (BxPC-3) and pancreatic stellate cell (HPSC) hybrid tumor-bearing nude mice, CRs exhibited improved immune escape ability, rapid extracellular matrix (ECM) penetration (8.2-fold higher than CSs), and enhanced tumor accumulation, further contributing to the enhanced antitumor efficacy. These findings may actually suggest the significance of shape design in improving current cell membrane-based drug delivery systems for effective subcellular targets and tumor therapy.


Subject(s)
Adenocarcinoma/drug therapy , Drug Delivery Systems , Nanoparticles/chemistry , Nanotubes/chemistry , Pancreatic Neoplasms/drug therapy , Adenocarcinoma/pathology , Animals , Cell Line, Tumor , Cell Membrane/chemistry , Cell Membrane/drug effects , Cell Shape/drug effects , Doxorubicin/chemistry , Doxorubicin/pharmacology , Drug Liberation , Endocytosis/drug effects , Endoplasmic Reticulum/drug effects , Endoplasmic Reticulum Stress/drug effects , Heterografts , Humans , Mice , Mice, Nude , Pancreatic Neoplasms/pathology , Pancreatic Stellate Cells/drug effects
17.
Pharmaceutics ; 11(2)2019 Feb 03.
Article in English | MEDLINE | ID: mdl-30717471

ABSTRACT

In this study, supercritical fluid (SCF) technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen (IBU) as a model compound. Solid-state characterization of the dispersions was conducted by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The PXRD and DSC results suggested that the amorphous form of IBU was maintained in the solid dispersions. Furthermore, in vitro dissolution and in vivo pharmacokinetic (PK) studies in rats were also performed. The dissolution performance of the SCF-prepared IBU dispersions was significantly improved compared to that of the physical mixtures of crystalline IBU and a polymer. In addition, the PK results revealed that the SCF-prepared IBU dispersions produced remarkably high blood drug concentrations (both the AUC and Cmax) and a rapid absorption rate (Tmax). Finally, molecular modeling was used to evaluate the binding energy of interactions between IBU and the polymers. The negative binding energy suggests a relatively stable system. Hence, SCF technology can be used as a very effective approach to prepare IBU solid dispersions with good physical stability and enhanced in vitro and in vivo performance.

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