Amount Of PLGA Research Articles

Multichannel 3D-printed bionanoparticles-loaded tablet (M3DPBT): designing, development, and in vitro functionality assessment

BackgroundThe intersubject variability which was related to the genetic makeup was the major cause of change in pharmacological and pharmacokinetic behavior of same dosage form in varied human being. 3D printing technology will help therapy evolve and eliminate the limitations of conventional technologies. Nebivolol's (NBL)-limited oral bioavailability is mainly due to its poor aqueous solubility. The research aims to combine advanced 3D printing technology and nanotechnology to design customized therapy and enhance the functionality of NBL using a statistical approach.Results and discussionThe results of the phase solubility indicated that NBL was a poorly aqueous soluble drug. Its solubility was increased by employing nanoparticle drug delivery, which is a promising solubility enhancement technique. The 32 full factorial design was employed to develop and optimize bionanoparticles (BNPs) by solvent evaporation technique using poly (lactic-co-glycolic acid 50:50) (PLGA 50:50) and poloxamer-407 as a surfactant. The BNPs were characterized by % encapsulation efficiency (% EE), Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimeter (DSC), transmission electron microscope (TEM), zeta potential, polydispersity index (PDI), particle size, in vitro drug release, etc. The BNPs loaded of NBL were further incorporated into the multichannel 3D-controlled release tablets made by PVA filaments employing fused deposition modeling (FDM) technology optimized by central composite design (CCD). Multichannel 3D-printed bionanoparticles-loaded tablet (M3DPBT) was optimized using CCD. All designed M3DPBTs were evaluated for post-fabrication parameters. The optimized M3DPBT could release more than 85% NBL within 10 h.ConclusionsThe newly fabricated M3DPBT was found stable. The amount of PLGA 50:50 and Polaxomer was significant for developing BNPs. % infill and layer height were observed as critical for the designing M3DPBT. The combined novel 3D printing and nanotechnology technology will open a new direction for patient compliance and better therapeutic effects.Graphical abstractDesigning and developing of M3DPBT is substantially improve the patient compliance and therapeutic effectiveness of Nebivolol.

Optimization and evaluation of a chitosan-coated PLGA nanocarrier for mucosal delivery of Porphyromonas gingivalis antigens

Recent advances in understanding Alzheimer's disease (AD) suggest the possibility of an infectious etiology, with Porphyromonas gingivalis emerging as a prime suspect in contributing to AD. P. gingivalis may invade systemic circulation via weakened oral/intestinal barriers and then cross the blood-brain barrier (BBB), reaching the brain and precipitating AD pathology. Based on the proposed links between P. gingivalis and AD, a prospective approach is the development of an oral nanovaccine containing P. gingivalis antigens for mucosal delivery. Targeting the gut-associated lymphoid tissue (GALT), the nanovaccine may elicit both mucosal and systemic immunity, thereby hampering P. gingivalis ability to breach the oral/intestinal barriers and the BBB, respectively.The present study describes the optimization, characterization, and in vitro evaluation of a candidate chitosan-coated poly(lactic-co-glycolic acid) (PLGA-CS) nanovaccine containing a P. gingivalis antigen extract. The nanocarrier was prepared using the double emulsion solvent evaporation method and optimized for selected experimental factors, e.g. PLGA amount, surfactant concentration, w1/o phase ratio, applying a d-optimal statistical design to target the desired physicochemical criteria for its intended application. After nanocarrier optimization, the nanovaccine was characterized in terms of particle size, polydispersity index (PdI), ζ-potential, encapsulation efficiency (EE), drug loading (DL), morphology, and in vitro release profile, as well as for mucoadhesivity, stability under simulated gastrointestinal conditions, antigen integrity, in vitro cytotoxicity and uptake using THP-1 macrophages.The candidate PLGA-CS nanovaccine demonstrated appropriate physicochemical, mucoadhesive, and antigen release properties for oral delivery, along with acceptable levels of EE (55.3 ± 3.5 %) and DL (1.84 ± 0.12 %). The integrity of the encapsulated antigens remained uncompromised throughout NPs production and simulated gastrointestinal exposure, as confirmed by SDS-PAGE and Western blotting analyses. Furthermore, the nanovaccine showed effective in vitro uptake, while exhibiting low cytotoxicity. Taken together, these findings underscore the potential of PLGA-CS NPs as carriers for adequate antigen mucosal delivery, paving the way for further investigations into their applicability as vaccine candidates against P. gingivalis.

Investigation of Alogliptin-Loaded In Situ Gel Implants by 23 Factorial Design with Glycemic Assessment in Rats.

The aim of the study was to design injectable long-acting poly (lactide-co-glycolide) (PLGA)-based in situ gel implants (ISGI) loaded with the anti-diabetic alogliptin. Providing sustained therapeutic exposures and improving the pharmacological responses of alogliptin were targeted for achieving reduced dosing frequency and enhanced treatment outputs. In the preliminary study, physicochemical characteristics of different solvents utilized in ISGI preparation were studied to select a proper solvent possessing satisfactory solubilization capacity, viscosity, water miscibility, and affinity to PLGA. Further, an optimization technique using a 23 factorial design was followed. The blood glucose levels of diabetic rats after a single injection with the optimized formulation were compared with those who received daily oral alogliptin. N-methyl-2-pyrrolidone (NMP) and dimethyl sulfoxide (DMSO), as highly water-miscible and low viscous solvents, demonstrated their effectiveness in successful ISGI preparation and controlling the burst alogliptin release. The impact of increasing lactide concentration and PLGA amount on reducing the burst and cumulative alogliptin release was represented. The optimized formulation comprising 312.5 mg of PLGA (65:35) and DMSO manifested a remarkable decrease in the rats’ blood glucose levels throughout the study period in comparison to that of oral alogliptin solution. Meanwhile, long-acting alogliptin-loaded ISGI systems demonstrated their feasibility for treating type 2 diabetes with frequent dosage reduction and patient compliance enhancement.

Pulmonary Delivery of Docetaxel and Celecoxib by PLGA Porous Microparticles for Their Synergistic Effects Against Lung Cancer.

Using a combination of chemotherapeutic agents with novel drug delivery platforms to enhance the anticancer efficacy of the drug and minimizing the side effects, is imperative to lung cancer treatments. The aim of the present study was to develop, characterize, and optimize porous poly (D, L-lactic-co-glycolic acid) (PLGA) microparticles for simultaneous delivery of docetaxel (DTX) and celecoxib (CXB) through the pulmonary route for lung cancer. Drug-loaded porous microparticles were prepared by an emulsion solvent evaporation method. The impact of various processing and formulation variables including PLGA amount, dichloromethane volume, homogenization speed, polyvinyl alcohol volume, and concentration, was assessed based on entrapment efficiency, mean release time, particle size, mass median aerodynamic diameter, fine particle fraction, and geometric standard deviation using a twolevel factorial design. An optimized formulation was prepared and evaluated in terms of size and morphology using a scanning electron microscope. FTIR, DSC, and XRD analyses confirmed drug entrapment and revealed no drug-polymer chemical interaction. Cytotoxicity of DTX along with CXB against A549 cells was significantly enhanced compared to DTX and CXB alone and the combination of DTX and CXB showed the greatest synergistic effect at a 1/500 ratio. In conclusion, the results of the present study suggest that encapsulation of DTX and CXB in porous PLGA microspheres with desirable features is feasible and their pulmonary co-administration would be a promising strategy for the effective and less toxic treatment of various lung cancers.

Investigating the Impact of Optimized Trans-Cinnamic Acid-Loaded PLGA Nanoparticles on Epithelial to Mesenchymal Transition in Breast Cancer.

PurposeTo design and optimize trans-cinnamic acid-loaded PLGA nanoparticles (CIN-PLGA-NPs) and assess its inhibitory effect on epithelial-mesenchymal transition (EMT) in triple-negative breast cancer.MethodsThe quality by design approach was used to correlate the formulation parameters (PLGA amount and Poloxamer188 concentration) and critical quality attributes (entrapment efficiency percent, particle size and zeta potential). Design of CIN-PLGA-NPs formulations was done based on central composite response surface design and formulated by nanoprecipitation method. In addition, the optimized CIN-PLGA-NPs formulation was further evaluated for morphology using transmission electron microscopy and in vitro dissolution test. The cytotoxicity of CIN-PLGA-NPs optimized formula in comparison to the free trans-cinnamic acid (CIN-Free) was investigated in vitro using MDA-MB-231, triple-negative breast cancer cells, followed by scratch wound assay for evaluating the impact on the migratory potential of MDA-MB-231 cells. In vivo antitumor activity was evaluated using Ehrlich ascites carcinoma solid tumor animal model where tumor volumes were measured at different time points and necrotic/apoptotic indices were estimated in tumor sections. EMT markers, E- and N-cadherin, were assessed in solid tumors as well.ResultsThe optimized formulation showed entrapment efficiency of 76.98%, particle size of 186.3 nm with a smooth spherical surface and zeta potential of −28.47 mV indicating its stability. Furthermore, CIN-PLGA-NPs optimized formula released 60.8±1.89% of the total CIN-Free within 24 hours compared to 29±1.25% of the raw CIN-Free indicating improved dissolution rate. The optimized formula showed superior cytotoxicity on MDA-MB-231 cells compared to its free counterpart as well as increased wound closure percentage along with reduced tumor size in mice and increased necrotic and apoptotic indices. Tumor levels of E-cadherin and N-cadherin were indicative of EMT inhibition.ConclusionOur findings proved the capability of PLGA nanoparticles in loading trans-cinnamic acid in addition to enhancing its antitumor efficacy in triple-negative breast cancer possibly via inhibiting EMT.

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of −29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.

Pharmacokinetics and in vivo distribution of optimized PLGA nanoparticles for pulmonary delivery of levofloxacin.

The aim of this study was to develop and optimize levofloxacin loaded PLGA nanoparticles (LN) for pulmonary delivery employing screening and experimental design and evaluate their in-vitro and in-vivo performance. The objective was to achieve Mass Median Aerodynamic Diameter (MMAD) of LN of less than 5μm, sustain the drug release up to 120 h and a higher AUC/MIC at the site of action. LN were prepared by modified emulsion solvent evaporation technique employing high speed homogenization, probe sonication and subsequent lyophilization. The Pareto chart from Placket Burman screening design revealed that homogenization speed and amount of PLGA were found to be significant (P < 0.05). Further analysis by 3 full-factorial design revealed that F-ratio was found to be far greater than the theoretical value (P < 0.05) for each regression model. The optimized formulation with desirability value 0.9612 showed mean particle size of 146 nm, MMAD of 4.40 μm and sustained the drug release up to 120 h in simulated lung fluid. Augmentation in Cmax (1.71-fold), AUC 0-∞ (5.46-fold), Mean Residence Time (6.64-fold) and AUC/MIC (6.21-fold) of LN through pulmonary route was found to significantly higher (P < 0.05) than levofloxacin (p. o.).

Lignin-Graft-Poly(lactic-co-glycolic) Acid Biopolymers for Polymeric Nanoparticle Synthesis.

A lignin-graft-poly(lactic-co-glycolic) acid (PLGA) biopolymer was synthesized with two types of lignin (LGN), alkaline lignin (ALGN) and sodium lignosulfonate (SLGN), at different (A/S)LGN/PLGA ratios (1:2, 1:4, and 1:6 w/w). 1H NMR and Fourier-transform infrared spectroscopy (FT-IR) confirmed the conjugation of PLGA to LGN. The (A/S)LGN-graft-PLGA biopolymers were used to form nanodelivery systems suitable for entrapment and delivery of drugs for disease treatment. The LGN-graft-PLGA NPs were generally small (100–200 nm), increased in size with the amount of PLGA added, monodisperse, and negatively charged (−48 to −60 mV). Small-angle scattering data showed that particles feature a relatively smooth surface and a compact spherical structure with a distinct core and a shell. The core size and shell thickness varied with the LGN/PLGA ratio, and at a 1:6 ratio, the particles deviated from the core–shell structure to a complex internal structure. The newly developed (A/S)LGN-graft-PLGA NPs are proposed as a potential delivery system for applications in biopharmaceutical, food, and agricultural sectors.

Antioxidant Activity and Hemocompatibility Study of Quercetin Loaded Plga Nanoparticles.

Quercetin (QU) is an important flavonoid compound presenting lots of biological activities, but its application has been limited due to its low aqueous solubility and instability. In this study, conducted to improve these properties of the quercetin, quercetin-encapsulated PLGA nanoparticles were prepared, characterized, and evaluated for antioxidant and hemolytic activity. Nanoparticles were produced by single emulsion solvent evaporation method. Four different process parameters initial QU amount, PVA concentration, PVA volume, and initial PLGA amount were investigated to obtain the nanoparticles which have minimum particle size and maximum entrapment efficiency. Synthesized nanoparticles were evaluated for particle size, entrapment efficiency, and reaction yield. Additionally, antioxidant properties and in-vitro hemolytic activity of quercetin loaded nanoparticles with different particle size were also evaluated for the first time in the literature. The antioxidant activity results showed that nanoparticles have different antioxidant activity, depending on the amount of quercetin release from nanoparticles at different particle sizes. The hemolytic activity results show that all nanoparticles exhibited favorable compatibility to red blood cells and no significant hemolytic effect was observed.

In vitro and in vivo evaluation of linezolid loaded electrospun PLGA and PLGA/PCL fiber mats for prophylaxis and treatment of MRSA induced prosthetic infections.

In this study, it was aimed to formulate linezolid loaded electrospun PLGA and PCL fiber mats doing controlled drug release, to be used in the treatment and prophylaxis of the prosthesis related infections. The effect of PLGA concentration, PLGA to PCL ratio and the amount of linezolid on the fiber and mat properties were examined. Fiber diameter has been shown to increase with increasing amount of PLGA and linezolid. Increase in PLGA amount resulted in reduced linezolid release, whereas increase in linezolid amount resulted in increased drug release. All PLGA fiber mats have shown to have favorable encapsulation efficiency (≥73%) and mechanical properties. Encapsulation efficiency and the mechanical properties deteriorated with the addition of PCL to the formulations. PLGA fiber mats have shown a biphasic controlled release and in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), pattern up to one month. The formulation selected as the optimum has been evaluated in vivo on the infected rats, which had prosthetic implantation after bone fracture. Consequently, it has been demonstrated microbiologically and histopathologically that a more efficient therapy and prophylaxis have been achieved with a 37-fold lower dose of linezolid.

Development and optimization of a novel PLGA-Levan based drug delivery system for curcumin, using a quality-by-design approach

This study aimed to develop a PLGA, Levan-based drug delivery system (DDS) of Curcumin using a quality-by-design (QbD) approach to reveal how formulation parameters affect the critical quality attributes (CQAs) of this DDS and to present an optimal design. First, a risk assessment was conducted to determine the impact of various process parameters on the CQAs of the DDS (i.e., average particle size, ZP, encapsulation efficiency and polydispersity index). Plackett–Burman design revealed that potential risk factors were Levan molecular weight, PLGA amount and acetone amount. Then, the optimization of the DDS was achieved through a Box–Behnken Design. The optimum formulation was prepared using low molecular weight Levan (134 kDa), 51.51 mg PLGA and 10 ml acetone. The model was validated and the optimized formulation was further characterized using different physic-chemical methods. The study resulted in the most stable NP with a spherical and uniform shape and physical stability tests indicated its stability for at least 60 days at room temperature. In conclusion, this study was an effort for developing a DDS which solubilizes Curcumin in clinically applicable concentrations.

Development of a fast and precise method for simultaneous quantification of the PLGA monomers lactic and glycolic acid by HPLC

Poly(lactide-co-glycolide acid) (PLGA) is an extraordinary well-described polymer and has excellent pharmaceutical properties like high biocompatibility and good biodegradability. Hence, it is one of the most used materials for drug delivery and biomedical systems, also being present in several US Food and Drug Administration-approved carrier systems and therapeutic devices. For both applications, the quantification of the polymer is inalienable. During the development of a production process, parameters like yield or loading efficacy are essential to be determined. Although PLGA is a well-defined biomaterial, it still lacks a sensitive and convenient quantification approach for PLGA-based systems. Thus, we present a novel method for the fast and precise quantification of PLGA by RP-HPLC. The polymer is hydrolyzed into its monomers, glycolic acid and lactic acid. Afterwards, the monomers are derivatized with the absorption-enhancing molecule 2,4′-dibromoacetophenone. Furthermore, the wavelength of the derivatized monomers is shifted to higher wavelengths, where the used solvents show a lower absorption, increasing the sensitivity and detectability. The developed method has a detection limit of 0.1 µg/mL, enabling the quantification of low amounts of PLGA. By quantifying both monomers separately, information about the PLGA monomer ratio can be also directly obtained, being relevant for degradation behavior. Compared to existing approaches, like gravimetric or nuclear magnetic resonance measurements, which are tedious or expensive, the developed method is fast, ideal for routine screening, and it is selective since no stabilizer or excipient is interfering. Due to the high sensitivity and rapidity of the method, it is suitable for both laboratory and industrial uses.

Optimization of PLGA-Resveratrol nanoparticle synthesis through combined response surface methodologies

Resveratrol is a natural phenol with anti-oxidant and anti-inflammatory activity, however it is limited by its in vivo low bioavailability and high metabolization rate. Its encapsulation in PLGA nanoparticles (NPs) can overcome such challenges. PLGA and PLGA-Resveratrol NPs optimal synthesis input variables were studied by fractional factorial and Box-Behnken design methodologies, respectively. It was found that PLGA NPs physicochemical properties were mainly affected by the amount of PLGA and PVA concentration. PLGA-Resveratrol NPs optimal synthesis, using as input variables the amount of PLGA, Resveratrol, and PVA concentration, yield a hydrodynamic diameter of 137 nm, polydispersity index of 0.195, drug loading of 16 %, and z-potential of -24.71 mV. These results are in very close agreement with the predicted values.

Preparation of Biodegradable Polymer Nanospheres Containing Manganese Porphyrin (Mn-Porphyrin)

Herein, poly(lactide-co-glycolide) (PLGA) nanospheres containing Mn-porphyrin, which exhibit chemically versatile and promising superoxide dismutase mimic, were prepared for biomaterial and drug-delivery-system formulations. The particle sizes and Mn-porphyrin-loading efficiencies of the nanospheres were controlled in order to realize breakthrough therapies for the incurable diseases. The sizes of the prepared Mn-porphyrin/PLGA nanospheres increased with the amount of PLGA used during preparation. Furthermore, the w1-to-o-phase volume ratio affected the loading efficiency of the Mn-porphyrin into the nanospheres. Nanospheres prepared from PLGA of lower molecular weight exhibited higher Mn-porphyrin-loading efficiencies. Furthermore, nanospheres prepared from PLGA with a molecular weight of 5000 exhibited a loading efficiency of 60%, which is higher than those generally reported for other nanospheres (~ 10%). Release testing revealed that the molecular weight of the PLGA influenced the release behaviour of the Mn-porphyrin from the nanospheres. Hence, Mn-porphyrin/PLGA nanospheres with controllable particle sizes, loading efficiencies, and release behaviour were prepared.

PLGA: From a classic drug carrier to a novel therapeutic activity contributor

Poly(lactic-co-glycolic acid) (PLGA) is well known for its biocompatibility and minimal toxicity. It is one of the most promising biodegradable polymeric drug delivery systems able to get endorsement from regulatory bodies to enter market. For many decades, PLGA has been functioning as an excipient, which by definition is pharmaceutically inert at a given dose of formulation. Lactate (one of the hydrolysis products of PLGA) has a key role in biochemical pathways and could improve physiological activities in certain illnesses by exerting therapeutic effects such as angiogenesis and promotion of healing. These activities, however, depend on the released amounts and metabolic clearance of lactate and route of formulation delivery. In the current commentary, along with several key notes on the lactate interactions, we would like to inform the PLGA research community that lactate (resulting from local delivery of physiologically significant amount of PLGA) may positively or negatively affect therapeutic efficacy of certain drugs. Hence, the excipient role of PLGA may be investigated for its potential pharmacological contributions in some biomedical applications.

Preparation and pre-clinical characterization of sustainedrelease ketoprofen implants for the management of pain and inflammation in osteoarthritis

Purpose: To prepare and evaluate sustained-release ketoprofen implants for prolonged drug release and activity.Methods: Ketoprofen implants were prepared with poly (lactic-co-glycolic acid) (PLGA) and chitosan in the form of tablets. The implants were analyzed for drug loading, thickness, hardness, swelling, in vitro drug release, as well as in vivo analgesic and anti-inflammatory activities.Results: The implants were round, smooth in appearance, uniform in thickness and showed no cracks or physical defects on the surface. Their friability was &lt; 1 % while drug content ranged from 89.98 ± 2.06 to 92.95 ± 1.65 %. In vitro drug release ranged from 70.23 to 92.04 % at the end of 5 days. Implants containing higher amounts of PLGA produced the highest swelling (40.24 ± 1.08 %). Implant IKT3 showed maximum analgesic activity (7.75 ± 1.00 s) and shortest time of maximum analgesia (2.5 h) in hot plate method. Inhibition of rat paw edema for IKT1, IKT2 and IKT3 was 79.95, 69.98 and 82.24 %, respectively, after 24 h.Conclusion: Ketoprofen-loaded implant IKT3 (4:4:2 ratio of PLGA, chitosan and ketoprofen) provides relatively quick onset and prolonged duration of analgesic effect. Thus, ketoprofen implants have a potential for development into therapeutic products for prolonged management of pain and inflammation in osteoarthritis.Keywords: Osteoarthritis, Ketoprofen implant, Prolonged analgesia, Poly(lactic-co-glycolic acid), Chitosan

Mechanical Properties and Degradability of Electrospun PCL/PLGA Blended Scaffolds as Vascular Grafts

In our study, the mechanical properties and degradability of vascular grafts made from poly(e-caprolactone) (PCL) and poly(lactic-co-glycolic acid) (PLGA) at different ratios were investigated. The results showed that the electrospun PCL/PLGA grafts possess good mechanical properties and biodegradability. The tensile and burst strength of the scaffolds met the demands of vascular grafts. In vitro degradation tests indicated that the degradation rate of the materials increased with the percentage of PLGA, and in vivo tests showed that increasing the amount of PLGA is an effective way to promote cell infiltration. Particularly, the electrospun PCL/PLGA blended scaffold with 10% PLGA exhibited a balance of mechanical and degradation properties, making it a promising tissue engineering material for vascular grafts.

Stealth lipid polymer hybrid nanoparticles loaded with rutin for effective brain delivery – comparative study with the gold standard (Tween 80): optimization, characterization and biodistribution

The blood–brain barrier is considered the leading physiological obstacle hindering the transport of neurotherapeutics to brain cells. The application of nanotechnology coupled with surfactant coating is one of the efficacious tactics overcoming this barrier. The aim of this study was to develop lipid polymer hybrid nanoparticles (LPHNPs), composed of a polymeric core and a phospholipid shell entangled, for the first time, with PEG-based surfactants (SAA) viz. TPGS or Solutol HS 15 in comparison with the gold standard Tween 80, aiming to enhance brain delivery and escape opsonization. LPHNPs were successfully prepared using modified single-step nanoprecipitation technique, loaded with the flavonoid rutin (RU), extracted from the flowers of Calendula officinalis L., and recently proved as a promising anti-Alzheimer. The effect of the critical process parameters (CPP) viz. PLGA amount, Wlecithin/WPLGA ratio, and Tween 80 concentration on critical quality attributes (CQA); entrapment, size and size distribution, was statistically analyzed via design of experiments, and optimized using the desirability function. The optimized CPP were maintained while substituting Tween 80 with other PEG-SAA. All hybrid particles exhibited spherical shape with perceptible lipid shells. The biocompatibility of the prepared NPs was confirmed by hemolysis test. The pharmacokinetic assessments, post-intravenous administration to rats, revealed a significant higher RU bioavailability for NPs relative to drug solution. Biodistribution studies proved non-significant differences in RU accumulation within brain, but altered phagocytic uptake among various LPHNPs. The present study endorses the successful development of LPHNPs using PEG-SAA, and confirms the prospective applicability of TPGS and Solutol in enhancing brain delivery.

Poly(lactic-co-glycolic acid) (PLGA) as Ion-Conducting Polymer for Biodegradable Light-Emitting Electrochemical Cells

The use of biocompatible and biodegradable materials in optoelectronics will enable the development of promising applications in the field of healthcare and environmental sensors as well as a more sustainable production of technology. Here, we present light-emitting electrochemical cells which utilize the biodegradable polymer poly(lactic-co-glycolic acid) (PLGA) to promote ionic conductivity in the active layer of light-emitting electrochemical cells. The device performance was analyzed in terms of the volume fraction of PLGA in the active layer blend as well as with respect to three different lactic:glycolic monomer ratios (85:15, 75:25, 65:35). In all three cases, adding PLGA to the active layer leads to an improvement of the turn-on voltage of up to 2 V compared to reference devices without PLGA. This can be attributed to an increase in ionic conductivity, which was determined by impedance spectroscopy. Increasing the relative amount of PLGA in the active layer shows that the improvement is ultimately...

Caffeic Acid Phenethyl Ester Loaded PLGA Nanoparticles: Effect of Various Process Parameters on Reaction Yield, Encapsulation Efficiency, and Particle Size

CAPE loaded PLGA nanoparticles were prepared using the oil in water (o/w) single emulsion solvent evaporation methods. Five different processing parameters including initial CAPE amount, initial PLGA amount, PVA concentration in aqueous phase, PVA volume, and solvent type were screened systematically to improve encapsulation of hydrophobic CAPE molecule, simultaneously minimize particle size, and raise the reaction yield. Obtained results showed that the encapsulation efficiency of the nanoparticles significantly increased with the increase of the initial CAPE amount (p &lt; 0.05) and particle size (p &lt; 0.05). Furthermore, the particle size is significantly influenced by initial polymer amount (p &lt; 0.05) and surfactant concentration (p &lt; 0.05). By the optimization of process parameters, the nanoparticles produced 70 ± 6% reaction yield, 89 ± 3% encapsulation efficiency, −34.4 ± 2.5 mV zeta potential, and 163 ± 2 nm particle size with low polydispersity index 0.119 ± 0.002. The particle size and surface morphology of optimized nanoparticles were studied and analyses showed that the nanoparticles have uniform size distribution, smooth surface, and spherical shape. Lyophilized nanoparticles with different CAPE and PLGA concentration in formulation were examined for in vitro release at physiological pH. Interestingly, the optimized nanoparticles showed a high (83.08%) and sustained CAPE release (lasting for 16 days) compared to nonoptimized nanoparticle.