Fast Release Research Articles

Eutectic Resolves Lysolipid Paradox in Thermoresponsive Liposomes.

A better molecular understanding of the temperature-triggered drug release from lysolipid-based thermosensitive liposomes (LTSLs) is needed to overcome the recent setbacks in developing this important drug delivery system. Enhanced drug release was previously rationalized in terms of detergent-like effects of the lysolipid monostearyl lysophosphatidylcholine (MSPC), stabilizing local membrane defects upon LTSL lipid melting. This is highly surprising and here referred to as the 'lysolipid paradox,' because detergents usually induce the opposite effect─they cause leakage upon freezing, not melting. Here, we aim at better answers to (i) why lysolipid does not compromise drug retention upon storage of LTSLs in the gel phase, (ii) how lysolipids can enhance drug release from LTSLs upon lipid melting, and (iii) why LTSLs typically anneal after some time so that not all drug gets released. To this end, we studied the phase transitions of mixtures of dipalmitoylphosphatidylcholine (DPPC) and MSPC by a combination of differential scanning and pressure perturbation calorimetry and identified the phase structures with small- and wide-angle X-ray scattering (SAXS and WAXS). The key result is that LTSLs, which contain the standard amount of 10 mol % MSPC, are at a eutectic point when they release their cargo upon melting at about 41 °C. The eutectic present below 41 °C consists of a MSPC-depleted gel phase as well as small domains of a hydrocarbon chain interdigitated gel phase containing some 30 mol % MSPC. In these interdigitated domains, the lysolipid is stored safely without compromising membrane integrity. At the eutectic temperature, both the MSPC-depleted bilayer and interdigitated MSPC-rich domains melt at once to fluid bilayers, respectively. Intact, fluid membranes tolerate much less MSPC than interdigitated domains─where the latter have melted, the high local MSPC content causes transient pores. These pores allow for fast drug release. However, these pores disappear, and the membrane seals again as the MSPC distributes more evenly over the membrane so that its local concentration decreases below the pore-stabilizing threshold. We provide a pseudobinary phase diagram of the DPPC-MSPC system and structural and volumetric data for the interdigitated phase.

Astaxanthin-loaded alginate-chitosan gel beads activate Nrf2 and pro-apoptotic signalling pathways against oxidative stress

Oxidative stress (OS) plays a crucial role in disease development. Astaxanthin (ATX), a valuable natural compound, may reduce OS and serve as a treatment for diseases like neurodegenerative disorders and cancer. Nuclear factor-erythroid 2-related factor 2 (Nrf2) regulates antioxidant enzymes and OS management. We evaluated ATX’s antioxidant activity via Alg-CS/ATX gel beads in vitro. ATX-encapsulated alginate-chitosan (Alg-CS/ATX) gel beads were synthesized and structurally/morphologically characterized by SEM, FT-IR, and XRD. Their biological effects were examined in human umbilical vein endothelial cells (HUVECs) treated with H2O2 through MTT assay, Annexin V/PI, cell cycle studies, and western blotting. Alg-CS effectively carried ATX, with high capacity and reduced pore size. Alg-CS/ATX displayed an 84% encapsulation efficiency, maintaining stability for 30 days. In vitro studies showed a 1.4-fold faster release at pH 5.4 than at neutral pH, improving ATX’s therapeutic potential. HUVECs treated with Alg-CS/ATX showed enhanced viability via increased Nrf2 expression. Alg-CS gel beads exhibit significant potential as a biocompatible vehicle for delivering ATX to combat OS with considerable opportunity for clinical applications.

Imaging of extracellular and intracellular ATP in pancreatic beta cells reveals correlation between glucose metabolism and purinergic signalling

Adenosine triphosphate (ATP) is a universal energy molecule and yet cells release it and extracellular ATP is an important signalling molecule between cells. Monitoring of ATP levels outside of cells is important for our understanding of physiological and pathophysiological processes in cells/tissues. Here, we focus on pancreatic beta cells (INS-1E) and test the hypothesis that there is an association between intra- and extracellular ATP levels which depends on glucose provision. We imaged real-time changes in extracellular ATP in pancreatic beta cells using two sensors tethered to extracellular aspects of the plasma membrane (eATeam3.10, iATPSnFR1.0). Increase in glucose induced fast micromolar ATP release to the cell surface, depending on glucose concentrations. Chronic pre-treatment with glucose increased the basal ATP signal. In addition, we co-expressed intracellular ATP sensors (ATeam1.30, PercevalHR) in the same cultures and showed that glucose induced fast increases in extracellular and intracellular ATP. Glucose and extracellular ATP stimulated glucose transport monitored by the glucose sensor (FLII12Pglu-700uDelta6). In conclusion, we propose that in beta cells there is a dynamic relation between intra- and extracellular ATP that depends on glucose transport and metabolism and these processes may be tuned by purinergic signalling. Future development of ATP sensors for imaging may aid development of novel approaches to target extracellular ATP in, for example, type 2 diabetes mellitus therapy.

The Non-Thermal Radio Emissions of the Solar Transition Region and the Proposal of an Observational Regime

The transition region is a very thin but most peculiar layer in the solar atmosphere located between the solar chromosphere and the corona. It is a key region for understanding coronal heating, solar eruption triggers, and the origin of solar winds. Here, almost all physical parameters (density, temperature, and magnetic fields) have the maximum gradient. Therefore, this region should be highly dynamic, including fast energy releasing and transporting, plasma heating, and particle accelerating. The physical processes can be categorized into two classes: thermal and non-thermal processes. Thermal processes can be observed at ultraviolet (UV) and extreme ultraviolet (EUV) wavelengths via multi-wavelength images. Non-thermal processes accelerate non-thermal electrons and produce radio emissions via the gyrosynchrotron mechanism resulting from the interaction between the non-thermal electrons and magnetic fields. The frequency range spans from several GHz to beyond 100 GHz, in great number of bursts with narrowband, millisecond lifetime, rapid frequency drifting rates, and being referred to as transition region small-scale microwave bursts (TR-SMBs). This work proposes a new type of Solar Ultra-wide Broadband Millimeter-wave Spectrometer (SUBMS) that can be used to observe TR-SMBs. From SUBMS observations, we can derive rich dynamic information about the transition region, such as information about non-thermal energy release and propagation, the flows of plasma and energetic particles, the magnetic fields and their variations, the generation and transportation of various waves, and the formation and evolution of the source regions of solar eruptions. Such an instrument can actually detect the non-thermal signals in the transition region during no flare as well as the eruptive high-energy processes during solar flares.

Progenesis in dicyemids

AbstractDicyemids (Phylum Dicyemida) are the most common and characteristic endosymbiont living in the renal sac of benthic cephalopod molluscs. Precocious development of a hermaphroditic gonad occurs in the larvae and smaller juveniles of 40 dicyemid species from 17 cephalopod species so far and is the usual phenomenon in dicyemids. Based on the developmental and morphological features of precocious individuals, progenesis (a form of heterochrony) is the appropriate term for such precocious development. In general, progenetic individuals have much lower fecundity than normal ones because of their smaller body size, and therefore, it appears to be a disadvantageous reproductive trait. Nonetheless, the number of progenetic individuals consists of 30%–50% of the population, a relatively large proportion suggesting that the presence of progenetic individuals probably plays an important role in life history strategy. Precocious development significantly reduces growth time and enables early maturation. Progenetic individuals are common in short‐living cephalopod species, in which precocious development seems appropriate for dicyemids, enabling fast larval release before the end of the host's life span.

Development of oral formulation of Lepidium seeds significantly decreases the high blood glucose levels in diabetic rats: in vitro formulation and in vivo antidiabetic performance

Background Lepidium sativum, Garden Cress (GC), seeds have a lot of natural molecules with a pronounced activity against different disorders. It was reported that GC seeds have the ability to lower the blood glucose level. Aim The aim of this work was to formulate GC seeds into oral tablets containing a fixed dose of the grounded seeds. Furthermore, the anti-diabetic performance of the prepared tablets was studied in the streptozotocin rats’ model in comparison with positive control metformin. Methods Micrometrics of GC grounded seeds with different excipients were investigated. Then, GC tablets were prepared via direct compression technique. GC tablets were characterized for their uniformity of dosage unit, friability, hardness, disintegration time, and in vitro release. The antidiabetic effect was studied in rats for a period of 28 days. Glycosylated hemoglobin, liver performance, and lipid levels include total cholesterol (TC), triglycerides (TGs), high-density lipoprotein (HDL), and low-density lipoprotein (LDL) were also estimated. In addition, histopathological study of liver and pancreas was also performed. Results Prosolv®EasyTab produced tablets with higher hardness, lower disintegration time, and fast release. GC tablets significantly lower the elevated blood glucose level. In addition, they have antihyperlipidemic activity, hepatocellular protective role and restore the histology of the liver and pancreas. Conclusion GC tablets could be a promising alternative formulation to control the high blood glucose level in diabetic rats rather than chemically derivatized drugs.

Effects of food to inoculum ratio and ultrasound pre-treatment on biogas production from dissolved air flotation waste from dairy industry

Dissolved air flotation (DAF) waste, a byproduct with high lipid content separated from dairy wastewater, is disposed of by land spreading and causing environmental pollution. To develop a sustainable treatment for DAF waste, this study investigated the effects of food to inoculum (F/I) ratio and ultrasound pre-treatment on the anaerobic digestion of DAF waste. The biochemical methane potential (BMP) of tested DAF waste ranged from 436–566 mL CH4/g VSfed. Increasing the F/I ratio (>1.0) inhibited methane production due to long chain fatty acids (LCFA) accumulation, which high concentrations of oleate inhibited methanogenesis and delayed palmitate degradation. Ultrasound pre-treatment with 30 min pulse (10 s on/ 10 s off) and 15 min continuous operations increased soluble chemical oxygen demand in DAF waste by 82% and 52%, respectively. Moreover, continuous sonication removed 38% of LCFA due to the implosion of cavitation bubbles. The BMP of DAF waste increased by 36% after sonication with F/I ratio 3.0. However, the lag time of methane production was prolonged after sonication due to the fast release of LCFA to the bulk solution. By implementing ultrasound pre-treatment and optimizing the F/I ratio, the energy potential of DAF waste can be harnessed, leading to more sustainable practices in dairy production.

Farmers’ perceptions on organic fertilisers towards circularity – a case study in Sweden

ABSTRACT Adequate treatment of organic manures and digestates from livestock production should reduce environmental impacts and provide well-defined and attractive biofertlisers for a crop production market, which can promote the closure of the nutrient cycle in agriculture. In this sense, a survey was conducted during the autumn of 2021 to investigate Swedish farmers’ perspectives on organic fertilisers use. The survey consisted of an online questionnaire, which was distributed broadly in the social media, homepages, different types of networks and at course events in order to reach all types of farms. There were 22 questions focused on current use, reasons for current use and preferences for future use. The analysis of the 99 fully responded surveys, demonstrated that 43% of the respondents think that they will increase their use of organic fertilisers in the coming 5–10 years and 60% think that they will use manure digestate in different forms (both solid and liquid fractions). Soil improvement was the main reason to use organic fertilisers, but there were also preferences for organic fertilisers with fast release of nutrients. The risk of soil compaction was the main reason not to use organic fertilisers and based on the responses, pellets and granulates seem to be more interesting than liquids and solids in general. Animal manures dominate the current use of organic fertilisers in Sweden however, other types of organic waste such as digestate and digestate derived fertilisers seems appealing to Swedish farmers. In conclusion, from this survey with 62% of the respondees in crop production, we found several indications of that there is a potential for increased use of organic fertilisers in Sweden on farms with limited use today. We found an openness, a broad interest and a demand for different types of products of different forms and origin. Since this demand in the end will almost always depend on the price of products in relation to the price of mineral fertilisers, which are fluctuating, we see the need of policy incentives in order to stimulate initiatives for the development towards increased circularity of nutrients.

Polyacrylic acid/polyvinylpyrrolidone/iron oxide nanocarrier for efficient delivery of doxorubicin

Recently, stimuli-responsive drug delivery systems (DDS), especially pH-responsive ones, have drawn a lot of attention to overcome the unfavourable side effects of traditional cancer treatments. In this work, a nanocomposite hydrogel based on polyacrylic acid (PAA), polyvinylpyrrolidone (PVP), and iron oxide (hematite, Fe2O3) nanoparticles was developed using the water/oil/water emulsification technique for the efficient delivery of doxorubicin (DOX) drug. The synthesized nanocarrier was characterized via XRD, and FT-IR to get information about its crystalline structure and the interaction between the functional groups of the different constituents, respectively. Its size distribution and colloidal stability were investigated via DLS and zeta potential tests, and morphological study was carried out by FE-SEM. The nanoparticles were found to be uniform and monodisperse, with an average size of 319 nm and a surface charge of −30.4 mV. The incorporation of hematite increased the drug loading (48.5 %) and encapsulation efficiency (86.57 %) due to its high porosity and surface area. Drug release was tested at pH 7.4 and 5.4, corresponding to healthy and cancerous tissues, and the results demonstrated the pH responsiveness of the system, with faster release (54 % in 24 h) in the acid medium. MTT and flow cytometry tests corroborated its strong anticancer effect since the nano-platform significantly reduced the survival rate of cancer cells. The designed pH-responsive platform holds great potential for breast cancer therapy.

Modelling functionalized drug release for a spherical capsule

Advances in material design have led to the rapid development of novel materials with increasing complexity and functions in bioengineering. In particular, functionally graded materials (FGMs) offer important advantages in various fields of application. In this work, we consider a heterogeneous reaction-diffusion model for an FGM spherical drug release system that generalizes the multi-layer configuration to arbitrary spatially-variable coefficients. Our model proposes a possible form for the drug diffusivity and reaction rate functions exhibiting fixed average material properties and a drug release profile that can be continuously varied between the limiting cases of a homogeneous system (constant coefficients) and two-layer system (stepwise coefficients). A semi-analytical solution is then used to solve the model, which provides closed-form expressions for the drug concentration and drug release profiles in terms of generalized Fourier series. Our results show how the release rate of the proposed FGM drug release system can be controlled and continuously varied between a fast (homogeneous) and slow (two-layer) release while maintaining the same averaged values for the diffusivity and reaction rate.

An easy approach towards once a day sustained release dosage form using microporous Cu-MOFs as drug delivery vehicles

Metal–organic frameworks (MOFs) have potential as drug carriers on the basis of their surface areas and pore volumes that allow for high drug loading and fast release.

The heterobivalent (SSTR2/albumin) radioligand [67Cu]Cu-NODAGA-cLAB4-TATE enables efficient somatostatin receptor radionuclide theranostics.

Somatostatin type 2 receptor (SSTR2) radionuclide therapy using β- particle-emitting radioligands has entered clinical practice for the treatment of neuroendocrine neoplasms (NENs). Despite the initial success of [177Lu]Lu‑DOTA-TATE, theranostic SSTR2 radioligands require improved pharmacokinetics and enhanced compatibility with alternative radionuclides. Consequently, this study evaluates the pharmacokinetic effects of the albumin-binding domain cLAB4 on theranostic performance of copper‑67-labeled NODAGA-TATE variants in an SSTR2-positive mouse pheochromocytoma (MPC) model. Methods: Binding, uptake, and release of radioligands as well as growth-inhibiting effects were characterized in cells grown as monolayers and spheroids. Tissue pharmacokinetics, absorbed tumor doses, and projected human organ doses were determined from quantitative SPECT imaging in a subcutaneous tumor allograft mouse model. Treatment effects on tumor growth, leukocyte numbers, and renal albumin excretion were assessed. Results: Both copper‑64- and copper‑67-labeled versions of NODAGA-TATE and NODAGA-cLAB4‑TATE showed similar SSTR2 binding affinity, but faster release from tumor cells compared to the clinical reference [177Lu]Lu‑DOTA-TATE. The bifunctional SSTR2/albumin-binding radioligand [67Cu]Cu‑NODAGA-cLAB4‑TATE showed both an improved uptake and prolonged residence time in tumors resulting in equivalent treatment efficacy to [177Lu]Lu‑DOTA-TATE. Absorbed doses were well tolerated in terms of leukocyte counts and kidney function. Conclusion: This preclinical study demonstrates therapeutic efficacy of [67Cu]Cu‑NODAGA-cLAB4‑TATE in SSTR2-positive tumors. As an intrinsic radionuclide theranostic agent, the radioligand provides stable radiocopper complexes and high sensitivity in SPECT imaging for prospective determination and monitoring of therapeutic doses in vivo. Beyond that, copper‑64- and copper‑61-labeled versions offer possibilities for pre- and post-therapeutic PET. Therefore, NODAGA-cLAB4-TATE has the potential to advance clinical use of radiocopper in SSTR2-targeted cancer theranostics.

Two-way photoswitching norbornadiene derivatives for solar energy storage.

Molecular photoswitches of norbornadiene (NBD) derivatives have been effectively applied in molecular solar-thermal energy storage (MOST) by photoisomerization of NBD to a quadricyclane (QC) state. However, a challenge of the NBD-based MOST system is the lack of a reversible two-way photoswitching process, limiting conversion from QC to thermal and catalytic methods. Here we design a series of NBD derivatives with a combination of acceptor and donor units to achieve two-way photoswitching, which can optically release energy by back-conversion from QC to NBD. Highly efficient photoconversion yields from NBD to QC and QC to NBD are up to 99% and 82%, respectively. The energy storage density of two-way photoswitching NBD is up to 312 J g-1 and optically controlled two-way photoswitching devices are demonstrated for the first time both in flow and in thin films, which illustrate a promising approach for fast and robust energy release in both solution and solid state.

Key technologies of two-phase pulse detonation combustor

The pulse detonation combustor is a new type of power device based on periodic high-temperature and high-pressure gas generated by detonation combustion as thrust. Due to its extremely fast heat release rate, detonation combustion has the characteristics of high thermal efficiency, low fuel consumption and low pollutant emissions. In recent years, relevant institutions have conducted extensive research on pulse detonation combustors. However, most research results focus on single studies where the fuel and oxidant are in the gas phase. Based on the vision of engineering application of pulse detonation combustors, the research progress of two key pulse detonation technologies, fuel atomization blending technology and rapid short-distance low-resistance detonation technology, as well as the research status of two-phase pulse detonation combustion based on kerosene are introduced. Regarding fuel atomization and blending technology, this paper mainly introduces the fuel atomization mechanism of two-phase detonation, fuel atomization technology and oil and gas blending technology. Regarding rapid short-distance low-resistance detonation technology, it mainly introduces obstacle-assisted detonation technology, spark plug ignition technology, hot jet ignition technology, pre-detonation tube ignition technology, shock wave focusing detonation technology and plasma ignition technology.

Synaptotagmin-9 in mouse retina.

Synaptotagmin-9 (Syt9) is a Ca2+ sensor mediating fast synaptic release expressed in various parts of the brain. The presence and role of Syt9 in retina is unknown. We found evidence for Syt9 expression throughout the retina and created mice to conditionally eliminate Syt9 in a cre-dependent manner. We crossed Syt9fl/fl mice with Rho-iCre, HRGP-Cre, and CMV-Cre mice to generate mice in which Syt9 was eliminated from rods (rodSyt9CKO), cones (coneSyt9CKO), or whole animals (CMVSyt9). CMVSyt9 mice showed an increase in scotopic electroretinogram (ERG) b-waves evoked by bright flashes with no change in a-waves. Cone-driven photopic ERG b-waves were not significantly different in CMVSyt9 knockout mice and selective elimination of Syt9 from cones had no effect on ERGs. However, selective elimination from rods decreased scotopic and photopic b-waves as well as oscillatory potentials. These changes occurred only with bright flashes where cone responses contribute. Synaptic release was measured in individual rods by recording anion currents activated by glutamate binding to presynaptic glutamate transporters. Loss of Syt9 from rods had no effect on spontaneous or depolarization-evoked release. Our data show that Syt9 acts at multiple sites in the retina and suggest that it may play a role in regulating transmission of cone signals by rods.

Long-lasting insecticidal activity in plants driven by chlorogenic acid-loaded metal-organic frameworks.

Metal-organic frameworks (MOFs) possess a variety of interesting features related to their composition and structure that make them excellent candidates to be used in agriculture. However, few studies have reported their use as delivery agents of agrochemicals. In this work, the natural polyphenol chlorogenic acid (CGA) was entrapped via simple impregnation in the titanium aminoterephthalate MOF, MIL-125-NH2. A combination of experimental and computational techniques was used to understand and quantify the encapsulated CGA in MIL-125-NH2. Subsequently, CGA delivery studies were carried out in water at different pHs, showing a fast release of CGA during the first 2 h (17.3 ± 0.3% at pH = 6.5). In vivo studies were also performed against larvae of mealworm (Tenebrio molitor), evidencing the long-lasting insecticidal activity of CGA@MIL-125-NH2. This report demonstrates the potential of MOFs in the efficient release of agrochemicals, and paves the way to their study against in vivo models.

Modulating Hydroxyl Adsorption on Transition Metal Nitrides by Magnetic Moments toward Fast Alkaline Hydrogen Evolution

Water dissociation is a critical step limiting the kinetics of electrocatalytic hydrogen evolution reaction (HER) in the alkaline. However, the effect of hydroxyl groups (OH*) on the electrocatalyst surface during the HER process has not been clarified yet. Here, three typical transition metal (TM) nitrides (i.e., Fe2N, Co3N and Ni3N) were investigated by combing theoretical calculation and experiments toward alkaline HER. The results show binding energy of OH* (∆EOH*) and magnetic moment of three nitrides follow the same trend of Fe2N > Co3N > Ni3N, showing a positive correlation. The as-synthesized Ni3N with the smallest magnetic moment shows the best alkaline HER activity due to its lowest water-dissociation barrier and weakest ∆EOH*. Weak adsorption to OH* could promote the fast release of OH* and thus enhance reaction kinetics. A small bond order corresponding to weak interaction between Ni3N and OH* is found to be favorable to the release of OH* and subsequent reaction steps, which originates from the orbital interaction of outer-shell electrons in TM and OH*. This work provides new insights into the design of advanced electrocatalysts using magnetic matrix toward alkaline HER.

Preparation of a novel alginate hydrogel microspheres covered by hollow silica for controlled-release application

Sodium alginate hydrogel has been widely used in the field of controlled-release. In this paper, in order to prevent the negative effect of fast degradation and explosive release of pure sodium alginate hydrogel in the drug delivery process, we developed a novel alginate hydrogel supported by hollow silica microsphere for drug delivery. Briefly, the drugs were fused with sodium alginate and the hollow silica microspheres followed by ion crosslinking to form a composite hydrogel microsphere with a core–shell structure (SA@SiO2). The structure and morphology of the composite hydrogel were characterized by Fourier infrared spectroscopy (FT-IR), thermogravimetric analysis (TG), scanning electron microscope (SEM), transmission electron microscope (TEM) along with fluorescence microscope. On this basis, using three different types of organic compounds (rhodamine B, Indocyanine green and salicylic acid) as model molecules, the controlled-release performance of the SA@SiO2 microspheres were investigated in detail. The research results show that the drug delivery system has broad-spectrum controlled-release performance for different types of molecules, and the controlled-release time can exceed 40 h. At the same time, the pH- responsive property of the sodium alginate hydrogel endows the delivery system with a certain targeting function. This study provides a new strategy for constructing an efficient targeted drug controlled-release system.

Magnetic nano composites for gallic acid delivery

A new magnetic layered double hydroxide (MLDH) composed of Fe, Mg, and Al was designed to improve gallic acid delivery to breast tumors. The metals formed the octahedrons within the layers, while the gallate ions were dissolved in the aqueous interlayer space. The drug loading was 30 %, determined with UV/Vis spectrophotometry. The material exhibited superparamagnetic behavior with a saturated magnetization of 5.5 emu/gr. This magnetic property enables the compound to be directed towards the therapeutic target using an external magnetic field, while the superparamagnetic attribute prevents the material from remaining magnetized in the body after the external magnetic field is removed. The diameter of the composites, measured from TEM images, was 110 nm: small enough for systemic circulation. For comparison, a conventional layered double hydroxide composed of Mg and Al was loaded with gallic acid and impregnated with Fe3O4 magnetic nanoparticles (LDH-NP). The drug loading was slightly lower (23 %), and the material demonstrated a combination of superparamagnetic and ferromagnetic behavior. However, the saturated magnetization was higher, 15 emu/gr for the superparamagnetic-like component and 13 emu/gr for the ferromagnetic-like component. From TEM images, the diameter of the composites was 57 nm. Drug release was studied with Franz diffusion cells. Both systems showed fast release at the lysosomal pH (4.8), but the MLDH avoids the release at the blood pH (7.4) more than the LDH-NP. Lastly, the systems were tested against breast cancer cells. After 48 h, the new composite demonstrated a 77 % reduction in cell viability, while the conventional composite impregnated with NPs showed a 66 % reduction. The designed Fe/Mg/Al magnetic nano composite loaded with gallic acid is easier to manufacture and holds promise for breast cancer treatments.

A Comparative Study of Influence of Different Polymers on Lumefantrine: Piperine Solid Dispersion

To improve the oral delivery of biopharmaceutical classification system (BCS) class II drugs, solid dispersions techniques are generally adopted in drug product develooment in pharmaceuticals. The choice of polymer in these designs significantly affects a drug’s solubility and dissolution properties. The crystalline nature and the involvement of P-glycoprotein in active ingredient efflux further hinder drug absorption and bioavailability. In this study, solid dispersion (SD) of an antimalarial drug (lumefantrine) combined with piperine (a P-gp and CYP3A4 inhibitor), was created using different polymeric carriers: Soluplus, Klucel, Poloxamer, Povidone/PVP K30 (PVP), and Copovidone/Kollidon® VA64 (KOL). Among these, LUMF-PIP solid dispersion with SOL exhibited the maximum water solvency and fastest release across various media. These findings indicate that the choice of polymeric carrier significantly impacts LUMF’s solubility and dissolution behavior in solid dispersion. SOL emerges as the most promising polymer for enhancing LUMF’s solubility and dissolution, ultimately leading to improved bioavailability upon oral administration.