Loaded Poly (lactic-co-glycolic) Acid Nanoparticles Research Articles

Investigation of cellular and molecular mechanisms of caffeic acid phenethyl ester loaded nanoparticle systems in breast cancer cell lines

Breast cancer is associated with high morbidity and mortality in women since conventional treatment methods are limited due to toxicity problems and inadequate targeting of cancer cells. The aim of this study is to develop caffeic acid phenethyl ester (CAPE) loaded polymeric nanoparticles to provide treatment for breast cancer and investigate their anti-tumor activity on MCF-7 and MDA-MB-231 breast cancer cells. CAPE was encapsulated into poly lactic-co-glycolic acid (PLGA) polymer using single-emulsion (o/w) solvent evaporation method and characterization of CAPE loaded PLGA nanoparticles (CAPE-NPs) were performed by particle size, zeta potential, polydispersity index, in vitro release profile, and surface morphology. CAPE-NPs were tested for cytotoxicity, anti-migration, anti-proliferation and apoptotic activities on breast cancer cells. The mean nanoparticle size was found as 196,1 ± 8982 nm and polydispersity index (PDI) was 0186 ± 0069. The results of the in vitro cell culture studies indicated that treatment of breast cancer cells with CAPE and CAPE-NPs inhibited cell viability and proliferation. IC50 values for 48 h were determined as 28.35 μg/ml,19.57 μg/ml for CAPE and CAPE-NP, respectively. Additionally, CAPE-NPs induced intrinsic pathway of apoptosis in MCF-7 and MDA-MB-231 cell lines. Overall, CAPE-NPs showed more efficient anti-tumour activity on breast cancer cells by small size and enhanced bioavability.

Vaccine-Induced Immunity Elicited by Microneedle Delivery of Influenza Ectodomain Matrix Protein 2 Virus-like Particle (M2e VLP)-Loaded PLGA Nanoparticles.

This study focused on developing an influenza vaccine delivered in polymeric nanoparticles (NPs) using dissolving microneedles. We first formulated an influenza extracellular matrix protein 2 virus-like particle (M2e VLP)-loaded with poly(lactic-co-glycolic) acid (PLGA) nanoparticles, yielding M2e5x VLP PLGA NPs. The vaccine particles were characterized for their physical properties and in vitro immunogenicity. Next, the M2e5x VLP PLGA NPs, along with the adjuvant Alhydrogel® and monophosphoryl lipid A® (MPL-A®) PLGA NPs, were loaded into fast-dissolving microneedles. The vaccine microneedle patches were then evaluated in vivo in a murine model. The results from this study demonstrated that the vaccine nanoparticles effectively stimulated antigen-presenting cells in vitro resulting in enhanced autophagy, nitric oxide, and antigen presentation. In mice, the vaccine elicited M2e-specific antibodies in both serum and lung supernatants (post-challenge) and induced significant expression of CD4+ and CD8+ populations in the lymph nodes and spleens of immunized mice. Hence, this study demonstrated that polymeric particulates for antigen and adjuvant encapsulation, delivered using fast-dissolving microneedles, significantly enhanced the immunogenicity of a conserved influenza antigen.

CFP10-loaded PLGA nanoparticles as a booster vaccine confer protective immunity against Mycobacterium bovis.

Introduction: The limited efficacy of BCG (bacillus Calmette-Guérin) urgently requires new effective vaccination approaches for the control of tuberculosis. Poly lactic-co-glycolic acid (PLGA) is a prevalent drug delivery system. However, the effect of PLGA-based nanoparticles (NPs) against tuberculosis for the induction of mucosal immune response is no fully elucidated. In this study, we hypothesized that intranasal immunization with culture filtrate protein-10 (CFP10)-loaded PLGA NPs (CFP10-NPs) could boost the protective immunity of BCG against Mycobacterium bovis in mice. Methods: The recombinant protein CFP10 was encapsulated with PLGA NPs to prepare CFP10-NPs by the classical water-oil-water solvent-evaporation method. Then, the immunoregulatory effects of CFP10-NPs on macrophages in vitro and on BCG-immunized mice in vivo were investigated. Results: We used spherical CFP10-NPs with a negatively charged surface (zeta-potential -28.5 ± 1.7 mV) having a particle size of 281.7 ± 28.5 nm in diameter. Notably, CFP10-NPs significantly enhanced the secretion of tumor necrosis factor α (TNF-α) and interleukin (IL)-1β in J774A.1 macrophages. Moreover, mucosal immunization with CFP10-NPs significantly increased TNF-α and IL-1β production in serum, and immunoglobulin A (IgA) secretion in bronchoalveolar lavage fluid (BALF), and promoted the secretion of CFP10-specific interferon-γ (IFN-γ) in splenocytes of mice. Furthermore, CFP10-NPs immunization significantly reduced the inflammatory area and bacterial load in lung tissues at 3-week post-M. bovis challenge. Conclusion: CFP10-NPs markedly improve the immunogenicity and protective efficacy of BCG. Our findings explore the potential of the airway mucosal vaccine based on PLGA NPs as a vehicle for targeted lung delivery.

Effect of Formulation Variables for the Production of WGA-Grafted, Levodopa-Loaded PLGA Nanoparticles

Levodopa is used for the treatment of Parkinson’s disease (PD) for the last few decades. However, adverse reactions such as dyskinesia, somnolence, nausea, itching, rash, as well as the need for frequent dosing and low bioavailability problems affect the success of the treatment. To prevent side effects caused by conventional therapy, a nanoparticular drug delivery system has been developed, in which receptors are constantly stimulated, and the frequency of dosing is reduced. In this study, levodopa was loaded in Poly lactic-co-glycolic acid (PLGA) nanoparticles (NP) which modified with Wheat Germ Agglutinin (WGA) To increase the effectiveness of levodopa, reduce its side effects and apply to the nasal area which is an alternative way for brain targeting with lower doses. To obtain the optimum levodopa loaded PLGA nanoparticles, the effect of some formulation variables such as polyvinyl alcohol (PVA) concentration, homogenization speed, polymer amount and molecular weight, and levodopa content on the entrapment efficiency (EE) and particle size of the nanoparticles were investigated. Besides these variables, the effect of different parameters on the WGA binding constant was also searched. In addition to in vitro release studies, Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectrophotometer (FT-IR), and Transmission electron microscopy (TEM) analysis were used in the characterization of nanoparticles. Among all formulations, A2 and A8a which was produced with different molcular weights of PLGA, different added levodopa amounts and with different homogenization speeds were chosen as optimum formulations due to their sustained release properties and the ability to release 80 % of their drug content.WGA binding constant was found 78.20 % for A8a-1 and 95 % for A2-1. In this study, we aimed to determine the effect of different formulation parameters on the development of levodopa loaded and WGA grafted PLGA nanoparticles and on the quality characteristics of nanoparticle formulations such as particle size, zeta potential, and EE. In this paper, our results are demonstrated for a better understanding of the effect of process parameters on the development of nanoparticle-based drug delivery systems by using the double-emulsion solvent evaporation technique and on WGA binding of drug-loaded PLGA nanoparticles.

PROCESS OPTIMIZATION USING QUALITY BY DESIGN (QBD) APPROACH OF A GENTAMICIN LOADED PLGA BIOCOMPOSITE

Osteomyelitis continues to be a major concern when orthopedic surgery is performed. Orthopedic infections have an incidence of 5% to 10% but their management proves to be quite difficult due to both biofilm formation and limited access of the drug to the infected area when systemic treatment is employed. The aim of the study was to optimize the synthesis process of a gentamicin loaded poly(-lactic-co-glycolic) acid (PLGA) based biodegradable composite by varying parameters that affect both efficiency encapsulation and nanoparticle size. Furthermore, a kinetic study was conducted to study the biodegradation process of the polymer. Gentamicin loaded PLGA nanoparticles were obtained using the double emulsion technique which allows the variation of several factors such as gentamycin concentration, PLGA concentration, buffer concentration and stirring speed. Out of the four factors evaluated, gentamicin concentration had the highest impact on both encapsulation efficiency and nanoparticle size. A few relevant interactions between factors were also registered.

Co-encapsulation of combinatorial flavonoids in biodegradable polymeric nanoparticles for improved anti-osteoporotic activity in ovariectomized rats

In our study a novel nanocombination of flavonoids was synthesized for anti-osteoporotic therapeutics. We chose 2 flavonoids, quercetin and curcumin to be encapsulated in polylactic-co-glycolic acid (PLGA) for anti-osteoporotic activity in induced ovariectomized rats. The synthesized flavonoids co-encapsulated PLGA nanoparticles were analysedfor morphological changes with electron micrography and its zeta potential along with PDI was determined. The encapsulation and loading efficiency studies were performed along with in vitro release studies. Cytotoxicity of the synthesized nanoparticles was evaluated with primary bone cells. The administration of the flavonoid co-encapsulated nanoparticles was done intragastrically after which the physical parameters of the femur, compression test of lumbar vertebra were studied. Weight of ash, % of ash and ash calcium of femoral bone were calculated along with biochemical characterization of serum. The histopathological examination of femur was done too. The synthesized flavonoids co-encapsulated PLGA nanoparticles were small enough (110–135 nm) and exhibited homogeneous distribution. The high encapsulation and loading efficiencies demonstrated a favourable nanocombination. The cytotoxicity results exhibited the cytocompatibility of the nanoparticles. From the in-vivo studies, it was seen that the flavonoids co-encapsulated PLGA nanoparticles inhibited trabecular bone loss and significantly improved bone mineral density and bone microarchitecture. The flavonoids loaded PLGA nanoparticles augmented the protective effect to prevent bone loss after ovariectomy. This study may be furthered for novel therapeutic management of osteoporosis. • Quercetin and curcumin encapsulated in PLGA nanoparticles. • Encapsulation and loading efficiency studies with in-vitro release. • in-vivo studies show inhibited trabecular bone loss and improved bone density. • The protective effect on bone loss got augmented after ovariectomy.

Characterisation of Preformulation Parameters to Design, Develop and Formulate Silymarin loaded PLGA Nanoparticles for Liver Targeted Drug Delivery

Silymarin, a flavonolignan,derived from Silybum marianum, family Asteraceae has long been used as a hepatoprotective remedy. Silymarin has cytoprotective activities due to its antioxidant property and free radical scavenging activity. It inhibits the binding of hepatotoxins to receptor sites, protects hepatocyte membranes, enhances liver parenchyma regeneration and increases glutathione levels. The pharmacokinetic studies of past three decades revealed that Silymarin has poor absorption, rapid metabolism especially by Phase II metabolism and ultimately poor oral bioavailability. Typical oral adult dose of Silymarin is 240-800mg /day .It is a non-lipophilic and poorly water soluble compound with water solubility of 0.04mg/ml. Only 20-30% of oral Silymarin is absorbed from gastrointestinal tract where it undergoes extensive entero-hepatic circulation. The advanced type of formulation like polymeric nanoparticles (PNPs) can be successfully utilised for bioavailability enhancement and targeting the Silymarin to hepatocytes. A controlled release PNP of Silymarin was prepared by solvent evaporation method using Poly Lactic-co-Glycolic Acid (PLGA) as biodegradable polymer. Prior to the development of this novel dosage form, it is very important to identify fundamental physical and chemical properties of the drug molecule and other divided properties of the drug powder. This data helps in many of the subsequent events and approaches towards the development of a better formulation. Preformulation studies included determination of solubility, moisture content, partition coefficient, melting point , powder properties like tapped density, bulk density, compressibility index, flow properties like angle of repose, excipient compatibility, entrapment efficiency, release profile of nanoparticles like dissolution, stability studies like effect of temperature and humidity and analysis by scanning Electron Microscopy.

Distinct endocytosis and immune activation of poly(lactic-co-glycolic) acidnanoparticles prepared by single- and double-emulsion evaporation.

Background: Poly(lactic-co-glycolic) acid (PLGA) nanoparticles can be prepared by emulsion-solvent-evaporation from o/w and w1/o/w2 emulsions. Aims: To elaborate similarities and differences regarding mechanical, morphologicaland physicochemical properties, as well as endocytosis and dose-dependent immune responses by primary human leukocytes between nanoparticles prepared by these two methods. Methods: Fluorescently labeled as well as TLR agonist (R848)-loaded PLGA nanoparticles were prepared via both single- and double-emulsion solvent evaporation. Results: Particles prepared by both methods were similar in chemical composition and surface charge but exhibited slight differences in size and morphology. Pronounced differences were found for loading, dissolution and mechanical properties. The particles were differently endocytosed by monocytes and induced qualitatively and quantitatively different immune responses. Conclusions: Variations in nanoparticle preparation can affect particle-derived immunological characteristics.

2,4-Dichlorophenoxyacetic Acid Loaded Polymeric Nanoparticle Synthesis and Its Effect on Biomass in Medicago sativa Cell Suspension Cultures

Nanoparticular systems, which have made great advances with the development of nanotechnology, have been used extensively recently in pesticide, herbicide plant growth regulators, fertilizer applications, gene transfer technologies and agriculture. It was aimed to synthesize and characterize 2,4-D loaded PLGA nanoparticles and investigate their biological activity in comparison with its free form. Here, the effects of 2,4-D loaded poly (lactic-co-glycolic) acid (PLGA) nanoparticles on biomass in Medicago sativa cell suspension cultures were investigated. Single emulsion solvent evaporation method is used in nanoparticle synthesis. As a result of the characterization of nanoparticles, 63.82% encapsulation efficiency, 60.73% reaction efficiency and 10.51% drug loading capacities were calculated. Particle size was measured as 181.7 ± 3.74 nm, zeta potential -18.3 ± 1.48 and polydispersity index as 0.081.
 Compared with the free 2,4-D molecule, it was observed that the addition of 2,4-D to the medium using the nanoparticles drug release system increased the growth of plant cells and the yield of biomass in M. sativa cell suspension cultures.

PLGA encapsulated γ-cyclodextrin-meropenem inclusion complex formulation for oral delivery

Meropenem (MER) is one of the last resort antibiotics used to treat resistant bacterial infections. However, the clinical effectiveness of MER is hindered due to chemical instability in aqueous solution and gastric pH, and short plasma half-life. Herein, a novel multi-material delivery system based on γ-cyclodextrin (γ-CD) and poly lactic-co-glycolic acid (PLGA) is demonstrated to overcome these challenges. MER showed a saturated solubility of 14 mg/100 mL in liquid CO2 and later it was loaded into γ-CD to form the inclusion complex using the liquid CO2 method. The γ-CD and MER inclusion complex (MER-γ-CD) was encapsulated into PLGA by the well-established double emulsion solvent evaporation method. The formation of the inclusion complex was confirmed using FTIR, XRD, DSC, SEM, and 1H NMR and docking study. Further, MER-γ-CD loaded PLGA nanoparticles (MER-γ-CD NPs) were characterized by SEM, DLS, and FTIR. The drug loading and entrapment efficiency for MER-γ-CD were 21.9 and 92. 2% w/w, respectively. However, drug loading and entrapment efficiency of MER-γ-CD NPs was significantly lower at up to 3.6 and 42.1% w/w, respectively. In vitro release study showed that 23.6 and 27.4% of active (non-degraded drug) and total drug (both degraded and non-degraded drug) were released from MER-γ-CD NPs in 8 h, respectively. The apparent permeability coefficient (Papp) (A to B) for MER, MER-γ-CD, and MER-γ-CD NPs were 2.63 × 10−6 cm/s, 2.81 × 10−6 cm/s, and 2.92 × 10−6 cm/s, respectively. For secretory transport, the Papp (B to A) were 1.47 × 10−6 cm/s, 1.53 × 10−6 cm/s, and 1.58 × 10−6 cm/s for MER, MER-γ-CD and MER-γ-CD NPs, respectively. Finally, the MER-γ-CD inclusion complex and MER-γ-CD NPs retained MER’s antibacterial activities against Staphylococcus aureus and Pseudomonas aeruginosa. Overall, this work demonstrates the significance of MER-γ-CD NPs to protect MER from gastric pH with controlled drug release, while retaining MER’s antibacterial activity.

Improved anticancer efficiency of Mitoxantrone by Curcumin loaded PLGA nanoparticles targeted with AS1411 aptamer

Objective(s): Mitoxantrone (MTX) is one of the most commonly used chemotherapeutic agents for treatment of different cancers. However, prolonged treatment with MTX results in unwanted side effects and drug resistant cancer cells. Combination therapies and exploiting of targeted nanoparticles have the potential of improving the efficiency of drug treatment as well as reducing the side effects. Curcumin (CUR) is a biological molecules with anticancer property. In this study, we investigated whether targeted PLGA (Poly Lactic-co-Glycolic Acid)–CUR nanoparticles (NPs) can reinforce the effect of MTX on breast cancer cells.Materials and Methods: PLGA NPs containing CUR targeted with AS1411 aptamer were prepared by single emulsion evaporation method. Physicochemical properties of NPs were investigated. The cytotoxicity of non-targeted and targeted NPs along with MTX was evaluated on MCF7, 4T1 and L929 cell lines. Results: The results showed that PLGA-CUR NPs were synthetized with an average encapsulation efficiency of 66% with a mean size of 186±3.2 nm. The drug release of curcumin from these NPs within 72h was about 59% in neutral medium and 90% in acidic medium. Interestingly, the combined treatment with PLGA-CUR-Apt and MTX inhibited the cancer cell's proliferation significantly more than the non-targeted nanoparticles, CUR and MTX-treated group alone. Conclusion: These results suggest that targeted PLGA-CUR nanoparticles may consider as a potential therapeutic contender in improving the efficacy of MTX in Breast cancer therapy.

Articular Cartilage- and Synoviocyte-Binding Poly(ethylene glycol) Nanocomposite Microgels as Intra-Articular Drug Delivery Vehicles for the Treatment of Osteoarthritis.

Intra-articular (IA) injection is an attractive route of administration for the treatment of osteoarthritis (OA). However, free drugs injected into the joint space are rapidly cleared and many of them can induce adverse off-target effects on different IA tissues. To overcome these limitations, we designed nanocomposite 4-arm-poly(ethylene glycol)-maleimide (PEG-4MAL) microgels, presenting cartilage- or synoviocyte-binding peptides, containing poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) as an IA small molecule drug delivery system. Microgels containing rhodamine B (model drug)-loaded PLGA NPs were synthesized using microfluidics technology and exhibited a sustained, near zero-order release of the fluorophore over 16 days in vitro. PEG-4MAL microgels presenting synoviocyte- or cartilage-targeting peptides specifically bound to rabbit and human synoviocytes or to bovine articular cartilage in vitro, respectively. Finally, using a rat model of post-traumatic knee OA, PEG-4MAL microgels were shown to be retained in the joint space for at least 3 weeks without inducing any joint degenerative changes as measured by EPIC-μCT and histology. Additionally, all microgel formulations were found trapped in the synovial membrane and significantly increased the IA retention time of a model small molecule near-infrared (NIR) dye compared to that of the free dye. These results suggest that peptide-functionalized nanocomposite PEG-4MAL microgels represent a promising intra-articular vehicle for tissue-localized drug delivery and prolonged IA drug retention for the treatment of OA.

Pharmacokinetic profile of chitosan modified poly lactic co-glycolic acid biodegradable nanoparticles following oral delivery of gentamicin in rabbits

Gentamicin (GM) is a well know antibiotic and drug of choice for various infections and is available in the form of parenteral and topical formulations. Gentamicin has no oral dosage form due to its enzymatic degradation and poor bioavailability. This study was designed to optimize controlled release oral dosage form of GM using poly lactic co-glycolic acid (PLGA) nanoparticles (NPs) which were surface modified with chitosan. Nanoparticles were characterized for size, potential, scanning electron microscopy and fourier transform infrared spectroscopy. Drug concentration in plasma samples was determined by microbiological assay against Bacillus subtilis (ATCC 9372). In vitro release pattern was studied and the best formulation was administered to healthy rabbits for pharmacokinetic studies. Various pharmacokinetic parameters determined for oral formulation were area under the curve (AUC) 43.2 ± 2.16 h.mg/L, volume of distribution (Vd) 1.54 ± 0.25 L, half-life phase-1 (t1/2α) 0.59 ± 0.12 h, mean residence time (MRT) 11.22 ± 0.42 h, time to reach maximum concentration (Tmax) 2.56 ± 0.09 h and maximum concentration (Cmax) was 3.49 ± 0.10 mg/L. It is concluded that chitosan modified GM loaded PLGA NPs has potential for oral absorption and can be used for achieving therapeutic benefits.

Recent advances in nanoscopic drug delivery systems for the treatment of glaucoma

AbstractNeuroprotection for glaucoma is still an unmet medical need and a proper drug delivery to the posterior segment of the eye is crucial. During the last decade, researchers have focussed their attention in the development of new drug delivery systems such as nanostructured lipid carriers, liposomes and polymeric nanoparticles. These nanoscopic systems overcome ocular barriers and provide a prolonged drug delivery on the target tissue avoiding adverse effects of the encapsulated drugs. During this course, recent advances and future perspectives in nanoscopic drug delivery systems for the treatment of glaucoma would be reviewed. Moreover, among several drug delivery systems, biodegradable polymeric nanoparticles have been proven to constitute a safe and suitable vehicle to encapsulate a wide range of drugs and be administrated as eye‐drops. Therefore, poly‐lactic‐co glycolic acid (PLGA) in addition to be biodegradable, biocompatible and non‐toxic, have demonstrated to be an effective drug carrier for ocular drug delivery. In this sense, Memantine loaded PLGA nanoparticles functionalized with polyethylene glycol (MEM‐NP) constitute a suitable neuroprotective strategy to increase MEM availability. MEM‐NP adminstered as eye‐drops confirmed to be safe, well‐tolerated and neuroprotective in an experimental glaucoma model. Nanoscopic systems could be the key for the efficient topical administration of neuroprotective compounds glaucoma treatment.

Sustained release olmesartan medoxomil loaded PLGA nanoparticles with improved oral bioavailability to treat hypertension

In the present study we have developed olmesartan medoxomil (OLM) loaded poly (lactic-co-glycolic) acid (PLGA) nanoparticles to improve the oral bioavailability of OLM. The nanoparticles of OLM-PLGA were prepared using simple one step electrospray method. The process was optimized for the flow rate, voltage applied and the distance between needle and collector. The developed OLM-PLGA was 527 ± 50.21 nm in size with low size distribution (0.261 ± 0.021). The entrapment efficiency of the particles was found to be 78.65 ± 4.31%. The scanning electron microscopy (SEM) studies also revealed the homogenous distribution of particle size with smooth surface. The particles were found to be stable with extended in-vitro release profile and the complete release was obtained in 72 h. The in-vivo pharmacokinetic studies after the oral administration of OLM-PLGA in rats revealed the significantly high Cmax (17.66 ± 3.64 μg/mL) and AUC (82.45 ± 7.15 μg/mL*h) in comparison with OLM-suspension Cmax (5.21 ± 1.12 μg/mL) and AUC (21.62 ± 4.41 μg/mL*h). The current study revealed that the OLM could be well encapsulated in OLM-PLGA which could address the bioavailability issue of OLM and enhance its potency in the treatment of hypertension.

Structural analysis, molecular dynamics and docking calculations of skin protective tripeptide and design, characterization, cytotoxicity studies of its PLGA nanoparticles

The main purpose of current study is to analyze the structural behaviour of a skin protective tripeptide Gly-His-Lys (GHK) with anti-oxidant and anti-cancer properties, design and characterize its nanoformulation by experimental and spectroscopic techniques to ensure its stability and enhance bioavailability and biocompatibility. GHK is extensively used as a cosmetic products for the therapy of skin and hair deformation. In this study the calculations on GHK were performed at DFT/B3LYP level of theory with the 6–311++G (d,p) basis set to obtain optimized geometry, HOMO-LUMO energy gap, MEP analysis and vibrational wavenumbers. The spectroscopic investigation of GHK tripeptide was performed experimentally through optical spectroscopic techniques (such as FT-IR, FT-IR-ATR and Micro-RAMAN) and compared with theoretical wavenumbers. The Potantial Energy Distributions (PED) of the normal modes of vibrations were also carried out with the help of GAR2PED program. By using molecular dynamics simulation, the stability of the GHK in water and methanol mediums have been simulated. To reveal the mechanism of interaction between GHK tripeptide and Fibroblast Growth Factor, the hydrogen bonding interactions are also investigated by Molecular docking calculations. Besides, GHK-loaded Poly Lactic-co-Glycolic Acid (PLGA) nanoparticles (NPs) were synthesized with double emission (water/oil/water) method, and characterized with Zeta Sizer, UV–Vis Spectrometry, Transmission Emission Microscope and FT-IR Spectrometry. Due to the encapsulation, the shifts in the wavenumbers occurring at the characteristic peaks of GHK in histidine, peptide and carboxyl groups were also examined. The encapsulation and loading efficiencies were determined as 94% and 4%, also the in vitro release profile was performed. Peptide loaded PLGA NPs which have a spherical morphology were visualized by TEM. In vitro cell culture studies of both peptide-loaded PLGA NPs and GHK tripeptide were studied and non-toxic effect on L929 cells were found. This study is a pioneer in the development and design of products with nano-drug formulations with better effectiveness and stability, especially in cosmetic products.

Formulation of Antimicrobial Tobramycin Loaded PLGA Nanoparticles via Complexation with AOT.

Tobramycin is a potent antimicrobial aminoglycoside and its effective delivery by encapsulation within nanoparticle carriers could increase its activity against infections through a combination of sustained release and enhanced uptake. Effective antimicrobial therapy against a clinically relevant model bacteria (Pseudomonas aeruginosa) requires sufficient levels of therapeutic drug to maintain a drug concentration above the microbial inhibitory concentration (MIC) of the bacteria. Previous studies have shown that loading of aminoglycoside drugs in poly(lactic-co-glycolic) acid (PLGA)-based delivery systems is generally poor due to weak interactions between the drug and the polymer. The formation of complexes of tobramycin with dioctylsulfosuccinate (AOT) allows the effective loading of the drug in PLGA-nanoparticles and such nanoparticles can effectively deliver the antimicrobial aminoglycoside with retention of tobramycin antibacterial function.

Assessment of the Physicochemical and Thermal Characterization of Biofield Energy Treated Polylactic-co-glycolic acid (PLGA)

Polylactic-co-glycolic acid (PLGA) is a biodegradable copolymer. It has many applications in the pharmaceuticals and biomedical industries, but its degradation and stability is a major concern. The objective of this study was to evaluate the influence of the Trivedi Effect® on the physicochemical and thermal properties of PLGA using modern analytical techniques. The PLGA sample was divided into control and Biofield Energy Treated parts. The control sample did not obtain the Biofield Energy Treatment, whereas the treated PLGA was received the Trivedi Effect®-Consciousness Energy Healing Treatment remotely by a renowned Biofield Energy Healer, Alice Branton. The particle size values of the treated PLGA were increased by 8.97%(d10), 8.79%(d50), 4.72%(d90), and 6.61%{D(4,3)}; thus, the surface area of treated PLGA was significantly decreased by 6.84% compared with the control sample. The latent heat of evaporation and fusion of the treated PLGA were significantly increased by 29.60% and 230.93%, respectively compared with the control sample. The residue amount was significantly increased by 21.99% in the treated PLGA compared to the control sample. The maximum thermal degradation temperature of the treated PLGA was increased by 2.30% compared with the control sample. It was concluded that the Trivedi Effect®-Consciousness Energy Healing Treatment might have generated a new form of PLGA which may show better powder flow ability, thermal stability, and minimize the hydrolysis of the ester linkages of PLGA. This improved quality of PLGA would be a better choice for the pharmaceutical formulations (i.e., the drug like simvastatin, amoxicillin, and minocycline loaded PLGA nanoparticles) and manufacturing of biomedical devices, i.e., grafts, sutures, implants, surgical sealant films, prosthetic devices, etc., in the industry using it as a raw material.

Design and Characterization of Apocynin Loaded PLGA Nanoparticles and their In vivo Efficacy in Hyperoxaluric Rats.

Apocynin has become a drug of choice in NADPH oxidase induced pathological conditions. Hyperoxaluria is one such pathological condition where NADPH oxidase is involved in eliciting renal injury. Recently apocynin has shown to reverse the transcriptome profile of the NADPH oxidaseassociated genes and reduced oxidative burden in hyperoxaluric animals. The poor solubility of this drug creates certain apprehensions about its bioavailability. PLGA (Poly Lactic co-Glycolic Acid) encapsulation of drug nanoparticles have showed to induce sustain release and henceforth enhance the efficiency and bioavailability of drugs. Therefore, the present study is aimed to envisage a novel approach of synthesizing apocynin doped PLGA nanoparticles. The PLGA nanoparticles (both unloaded and loaded) were prepared using solvent extraction method and analyzed for size and stability by Dynamic Light Scattering (DLS), TEM (transmission electron microscopy) and zeta potential. Furthermore, the drug release and encapsulation efficiency of the drug was calculated in vitro. The nanoencapsulation formed was stable with desired size (217-259 nm) and posses a controlled drug release of 20%. Further this nanoencapsulation was explored for its potential to reduce hyperoxaluric manifestations in rats given ethylene glycol with ammonium chloride for 9 days. In comparison to free apocynin, it was found that nanoparticles containing apocynin showed moderately better results in vivo by maintaining serum urea and createnine levels. These nanoparticles can be used in diseases where a sustained release of apocynin is required.

Garlic oil–loaded PLGA nanoparticles with controllable size and shape and enhanced antibacterial activities

ABSTRACTThe present work focuses on producing polymer composite nanoparticles (NPs) composed of garlic oil (GO) and poly(lactic‐co‐glycolic) acid (PLGA) by the single emulsion/solvent evaporation (SE/SE) method and high‐speed homogenizing. Different preparation parameters were found to greatly affect the stability and size uniformity of the prepared PLGA/GO NP formulations, which were carefully controlled. Scanning electron microscopy, Fourier transform infrared spectroscopy, and UV–vis spectroscopy and dynamic light scattering and zeta potential were used to characterize the NPs. Antibacterial assessment of the prepared PLGA/GO NPs against E. coli and S. aureus was carried out. Interestingly, the NP size ranged between 201 and 319 nm, which is 10 times less than the size of the regular GO particles in bulk solution. The antibacterial activities show enhancement by 70–78% of bacterial inhibition compared with a GO bulk solution. This work sheds light on the potential use of GO NP formulations as nanobiotics and the critical NP preparation parameters that need to be considered. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018, 135, 46133.