Incorporation, Release, and Effectiveness of Dexamethasone in Poly(Lactic-Co-Glycolic Acid) Nanoparticles for Inner Ear Drug Delivery

2011 ◽  
Vol 2 (1) ◽  
Author(s):  
Youdan Wang ◽  
Xinsheng Gao ◽  
Satish Kuriyavar ◽  
David Bourne ◽  
Brian Grady ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Inner Ear ◽  
Cell Damage ◽  
Release Kinetics ◽  
Drug Loading ◽  
Superparamagnetic Iron Oxide ◽  
Plga Nanoparticles ◽  
Submicron Particles ◽  
Loading Efficiency

Poly (D,L-lactide-co-glycolide) (PLGA) particles have been widely used as drug delivery carriers for a variety of payloads. Three forms of dexamethasone (DEX), namely, acetate, base, and phosphate, were incorporated into a PLGA matrix. First, we compared the drug loading efficiency and release kinetics of drug-loaded PLGA particles. Dexamethasone acetate (DEX-Ac) loaded particles exhibited a higher loading efficiency and a more linear release profile of drug as compared with the other forms of DEX particles. Also, we coincorporated oleic acid-coated superparamagnetic iron oxide nanoparticles (SPION) with DEX-Ac into PLGA submicron particles. No differences in size, zeta potential, drug loading, or release kinetics were found between particles prepared with and without SPION. Additionally, particles were applied to an in vitro cochlear, organotypic culture. DEX-Ac PLGA nanoparticles showed a protective effect against 4-hydroxynonenal induced hair cell damage. These results suggest a promising method for inner ear magnetic targeted treatment.

scholarly journals SYNTHESIS AND CHARACTERIZATION OF THIOLATED JACKFRUIT SEED STARCH AS A COLONIC DRUG DELIVERY CARRIER

2019 ◽  
pp. 53-62 ◽  
Author(s):  
Sanjoy Das ◽  
Malay K. Das
Keyword(s):  
Drug Delivery ◽  
Release Kinetics ◽  
Drug Loading ◽  
Local Treatment ◽  
Entrapment Efficiency ◽  
Esterification Reaction ◽  
Compatibility Study ◽  
Mice Model ◽  
Drug Delivery Carrier

Objective: Site-specific drug delivery into the colonic region is extremely fascinating for local treatment of various colonic diseases like ulcerative colitis, colon cancer but it should be capable of saving the drug from hydrolysis and degradation. The present study reports the application of jackfruit seed starch and its thiol derivative as a drug delivery carrier for the colon. Methods: The starch was extracted from the jackfruit seeds by water extraction method and modified by the esterification reaction with thioglycolic acid. The thiolated starch was characterized for morphology, functional and flow properties. The safety profile of the thiolated starch was confirmed by acute toxicity study in a mice model as per OECD guidelines 423. The microspheres based on thiolated starch were prepared by ionic gelation method incorporating Ibuprofen as a model drug. The prepared microspheres were characterized for particle size, drug entrapment efficiency, drug loading, compatibility study, surface morphology, in vitro drug release and release kinetics. Results: The result attributed that starch was successfully modified by the thiolation with a degree of substitution of 3.30. The size of prepared microspheres ranges from 825.5±4.58 to 857±6.24 µm, the entrapment efficiencies ranges from 69.23±1.19 to 76.15±0.83 % and the drug loading capacity ranges from 17.75±0.30 to 46.05±0.49 %. The FT-IR, DSC and XRD studies confirmed that there is no interaction within drug and excipients. The thiolated starch microspheres show the maximum release of drug at pH 7.4 in the presence of rat caecal content as compared to pH 1.2 and pH 6.8 for up to 24 h and are following first order release kinetics. Conclusion: These results suggest the application of thiolated jackfruit seed starch could be promising as a long-term drug delivery carrier for the colon.

scholarly journals Electrospun poly (L-lactic acid)/gelatin membranes loaded with doxorubicin for effective suppression of glioblastoma cell growth in vitro and in vivo

2021 ◽  
Author(s):  
Boxun Liu ◽  
Zhizhong Jin ◽  
Haiyan Chen ◽  
Lun Liang ◽  
Yao Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Lactic Acid ◽  
Release Kinetics ◽  
Drug Loading ◽  
Composite Membranes ◽  
Spectroscopic Techniques ◽  
Loading Process

Abstract Electrospun membranes are attracting interest as a drug delivery system because of their material composition flexibility and versatile drug loading. In this study, the electrospun membrane was loaded with doxorubicin (DOX) via electrostatic adsorption for long-term drug delivery. DOX loading process was optimized by varying temperature, time, drug concentration, pH, and ionic strength of solutions. The loading process did not impair the structural properties of the membrane. Next, we investigated the drug release kinetics using spectroscopic techniques. The composite membranes released 22% of the adsorbed DOX over the first 48 h, followed by a slower and sustained release over 4 weeks. The DOX release was sensitive to acidic solutions that the release rate at pH 6.0 was 1.27 times as that at pH 7.4. The DOX-loaded membranes were found to be cytotoxic to U-87 MG cells in vitro that decreased the cell viability from 82.92% to 25.49% from 24 h to 72 h of co-incubation. These membranes showed strong efficacy in suppressing tumour growth in vivo in glioblastoma-bearing mice that decreased the tumour volume by 77.33% compared to blank membrane-treated group on Day 20. In conclusion, we have developed an effective approach to load DOX within a clinically-approved poly (L-lactic acid)/gelatin membrane for local and long-term delivery of DOX for the treatment of glioblastoma.

PLGA Nanoparticles for Anti Tuberculosis Drug Delivery

2012 ◽  
Vol 584 ◽  
pp. 465-469 ◽  
Author(s):  
S. Malathi ◽  
S. Balasubramanian
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Double Emulsion ◽  
Plga Nanoparticles ◽  
Release Mechanism ◽  
Sustained Drug Release ◽  
Drug Release Kinetics ◽  
Evaporation Technique

Nanoparticles-based drug delivery systems have considerable potential for the treatment of tuberculosis (TB). A series of PLGA polymers with different molar feed ratios (P2:87/13, P3:83/17, P5:63/37, P6:76/24, P9:53/47) were synthesized by direct melt poly condensation method. The resulting biodegradable polymers were characterized by FTIR and 1H NMR spectroscopy. The preparation of the drug (Pyrazinamide (PZA)) encapsulated PLGA polymers were carried out by double emulsion – solvent evaporation technique. The drug loaded PLGA-NPs were analyzed by UV-visible spectroscopy and scanning electron microscopy. The drug loading efficiency and drug release kinetics varies in the following order: P9>P5>P6>P3>P2. Among the formulations, PP9 showed a uniform as well as sustained drug release. The drug release kinetics has been evaluated by Zero-order, First order, Higuchi and Koresmeyer- Peppas models and the release mechanism has also been investigated

scholarly journals Polymer-free corticosteroid dimer implants for controlled and sustained drug delivery

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Kyle Battiston ◽  
Ian Parrag ◽  
Matthew Statham ◽  
Dimitra Louka ◽  
Hans Fischer ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Inflammatory Responses ◽  
Release Kinetics ◽  
Drug Loading ◽  
Rabbit Model ◽  
Drug Carriers ◽  
Surface Erosion ◽  
Sustained Drug Delivery

AbstractPolymeric drug carriers are widely used for providing temporal and/or spatial control of drug delivery, with corticosteroids being one class of drugs that have benefitted from their use for the treatment of inflammatory-mediated conditions. However, these polymer-based systems often have limited drug-loading capacity, suboptimal release kinetics, and/or promote adverse inflammatory responses. This manuscript investigates and describes a strategy for achieving controlled delivery of corticosteroids, based on a discovery that low molecular weight corticosteroid dimers can be processed into drug delivery implant materials using a broad range of established fabrication methods, without the use of polymers or excipients. These implants undergo surface erosion, achieving tightly controlled and reproducible drug release kinetics in vitro. As an example, when used as ocular implants in rats, a dexamethasone dimer implant is shown to effectively inhibit inflammation induced by lipopolysaccharide. In a rabbit model, dexamethasone dimer intravitreal implants demonstrate predictable pharmacokinetics and significantly extend drug release duration and efficacy (>6 months) compared to a leading commercial polymeric dexamethasone-releasing implant.

RESEALED ERYTHROCYTES: A PROMISING APPROACH TO ENHANCE EFFICACY OF ANTICANCER DRUGS

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (03) ◽  
pp. 9-20
Author(s):  
◽  
Prathibha Salve ◽  
Rajendra Doijad ◽  
Niranjan Chivate
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Anticancer Drugs ◽  
Delivery System ◽  
Release Kinetics ◽  
Drug Loading ◽  
The Body ◽  
Zero Order Release

Targeted drug delivery system is a potential drug delivery system which delivers the drug to particular organ of interest only. This improves the therapeutic efficacy of the treatment by reducing the side effects of drug which are required in case of anticancer drugs. Erythrocytes have been the most interesting carrier and have found to possess great potential in drug targeting. Resealed erythrocytes are gaining more popularity because of their ability to circulate throughout the body, biocompatibility, zero order release kinetics, reproducibility and ease of preparation. In this review, we have made an attempt to understand the process in detail to prepare resealed erythrocytes, including its mechanism, source and isolation of erythrocytes, methods of drug loading, in vivo and in vitro characterization of resealed erythrocytes, with special emphasis on applications of resealed erythrocytes for cancer treatment. With this review we can conclude that resealed erythrocyte is a promising approach to enhance efficacy of anticancer drugs.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

Minocycline hydrochloride loaded mPEG-PCLA membranes: Preparation and in vitro evaluation for periodontitis therapy

2021 ◽  
pp. 088391152199279
Author(s):  
Ningtao Wang ◽  
Zhengmei Huang ◽  
Shenchun Wang ◽  
Meidong Lang ◽  
Xiuyin Zhang
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Membrane Surface ◽  
Local Treatment ◽  
In Vitro Release ◽  
Periodontal Pathogen ◽  
Antibacterial Drug ◽  
Periodontal Ligament Fibroblasts ◽  
Minocycline Hydrochloride

This study was aimed at alleviating shortcomings in the treatment of periodontitis by preparation of a biopolymer membrane loaded with minocycline hydrochloride (MH) inserted into periodontal pockets to treat infections. Monomethoxy-poly (ethylene glycol)-poly (ε-caprolactone-co-L-lactide) (mPEG-PCLA) is a biocompatible and biodegradable amphiphilic block copolymer. It, therefore, has attracted considerable attention in drug delivery systems and periodontal treatment. We chose it as a membrane material for MH-drug loading. The MH-loaded membranes were prepared by the solvent casting technique with the content of 5, 8 and 10 wt.%, respectively. Fourier transform infrared spectra (FTIR) revealed no interaction between MH and polymer. The drug-loaded membrane surface morphology was investigated by scanning electron microscopy (SEM). In vitro release studies showed that the initial drug release exceeded 40% within 24 h, followed by a sustained release for up to 2 weeks, which would enable the therapeutic level to maintain over a longer time. The antibacterial activity studies in vitro demonstrated a positive effect on the periodontal pathogen. MH drug-loaded membranes have no adverse effect on the growth of periodontal ligament fibroblasts in the MTT test. The study suggests that mPEG-PCLA membranes containing MH are a potential antibacterial drug delivery system for local treatment of periodontitis.

scholarly journals pH-Responsive Release of Ruthenium Metallotherapeutics from Mesoporous Silica-Based Nanocarriers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 460
Author(s):  
Minja Mladenović ◽  
Ibrahim Morgan ◽  
Nebojša Ilić ◽  
Mohamad Saoud ◽  
Marija V. Pergal ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Inductively Coupled Plasma ◽  
Drug Delivery Systems ◽  
Mesoporous Silica Nanoparticles ◽  
Release Kinetics ◽  
Delivery Systems ◽  
Emission Spectrometry ◽  
Ph Responsive

Ruthenium complexes are attracting interest in cancer treatment due to their potent cytotoxic activity. However, as their high toxicity may also affect healthy tissues, efficient and selective drug delivery systems to tumour tissues are needed. Our study focuses on the construction of such drug delivery systems for the delivery of cytotoxic Ru(II) complexes upon exposure to a weakly acidic environment of tumours. As nanocarriers, mesoporous silica nanoparticles (MSN) are utilized, whose surface is functionalized with two types of ligands, (2-thienylmethyl)hydrazine hydrochloride (H1) and (5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)hydrazine (H2), which were attached to MSN through a pH-responsive hydrazone linkage. Further coordination to ruthenium(II) center yielded two types of nanomaterials MSN-H1[Ru] and MSN-H2[Ru]. Spectrophotometric measurements of the drug release kinetics at different pH (5.0, 6.0 and 7.4) confirm the enhanced release of Ru(II) complexes at lower pH values, which is further supported by inductively coupled plasma optical emission spectrometry (ICP-OES) measurements. Furthermore, the cytotoxicity effect of the released metallotherapeutics is evaluated in vitro on metastatic B16F1 melanoma cells and enhanced cancer cell-killing efficacy is demonstrated upon exposure of the nanomaterials to weakly acidic conditions. The obtained results showcase the promising capabilities of the designed MSN nanocarriers for the pH-responsive delivery of metallotherapeutics and targeted treatment of cancer.

Photodynamic Treatment of Colorectal Cancer Using Chlorin e6-Loaded Poly(lactide-co-glycolide)- Based Nanoparticles

2021 ◽  
Vol 17 (10) ◽  
pp. 1939-1950
Author(s):  
Beibei Lin ◽  
Xuegu Xu ◽  
Xiaobi Zhang ◽  
Yinfei Yu ◽  
Xiaoling Wang
Keyword(s):  
Colorectal Cancer ◽  
Drug Loading ◽  
Average Diameter ◽  
Plga Nanoparticles ◽  
Chlorin E6 ◽  
Photodynamic Treatment ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
The Stability

We prepared poly(lactide-co-glycolide) (PLGA) encapsulated with chlorin e6 (Ce6) in an effort to increase the stability and efficiency of photosensitizers for photodynamic therapy (PDT). We determined that Ce6-loaded PLGA nanoparticles (PLGA-Ce6 NPs) had drug-loading efficiency of 5%. The efficiency of encapsulation was 82%, the zeta potential was- 25 mV, and the average diameter was 130 nm. The encapsulation of Ce6 in PLGA nanoparticles showed excellent stability. The nanoparticles exhibited sustained Ce6 release profiles with 50% released at the end of 3 days, whereas free Ce6 showed rapid release within 1 day. Ce6 release patterns were controlled by encapsulation into PLGA. The uptake of PLGA-Ce6 NPs was significantly enhanced by endocytosis in the first 8 hours in the HCT-116 cell line. An intracellular reactive oxygen species assay revealed the enhanced uptake of the nanoparticles. An in vitro anti-tumor activity assay showed that the PLGA-Ce6 NPs exhibited enhanced phototoxicity toward HCT-116 cells and a slightly lower IC50 value in HCT-116 cells than Ce6 solution alone. Exposure of HCT-116 cell spheroids to PLGA-Ce6 NPs penetrated more profoundly and had better phototoxicity than pure drugs. These findings suggest that PLGA-Ce6 NPs might serve as PDT for colorectal cancer.

Therapeutic Properties of PDMS Nanoparticles: A Promising New Drug Delivery Vehicle Against Inflammatory Conditions

2021 ◽  
Vol 24 ◽  
Author(s):  
Aiswarya Anilkumar Ajitha ◽  
Sri SivaKumar ◽  
Gayathri Viswanathan ◽  
Sabulal Baby ◽  
Prabath Gopalakrishnan Biju
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
Release Kinetics ◽  
Drug Loading ◽  
Systemic Circulation ◽  
Biological Evaluation ◽  
Raw 264.7 Cells ◽  
Morphological Examination ◽  
Inflammatory Conditions ◽  
Anti Inflammatory

Background: Over the last few decades, there has been a stupendous change in the area of drug delivery using particulate delivery systems, with increasing focus on nanoparticles in recent times. Nanoparticles helps to improve and alter the pharmacodynamic properties and pharmacokinetics of various types of drug molecules. These features help to protect the drug entity in the systemic circulation, access of the drug to the chosen sites, and to deliver the drug in a controlled and sustained rate at the site of action. Objective: Nanoparticle based targeted delivery of anti-inflammatory drugs/signal modulatory agents to the cytoplasm or nuclei of the targeted cell can significantly enhance the precision and efficacy of intended therapeutic activity. To this end, we report ligand free, enhanced intra-nuclear delivery model of anti-inflammatory therapeutics via PDMS nanoparticles. Method: PDMS nanoparticles were prepared by sacrificial silica template-based approach and details of their characterization for suitability as a nanoparticle-based delivery material is detailed herein. Results: Biological evaluation for compatibility was carried out and the results showed that the PDMS nanoparticle has no toxicity on RAW 264.7 cells in the concentration range of 10, 20, 40, 60, 80, 100 and 120 μg/mL in culture. Biocompatibility and absence of toxicity was determined by morphological examination and cell viability assays. Drug loading and release kinetics were carried out with the anti-inflammatory drug Diclofenac. Conclusion: In this paper we clearly demonstrate the various aspects of nanoparticle articulation, characterization, effect of their characteristics and their applications as a non-toxic drug delivery molecule for its potential applications in therapeutic delivery of drugs for sustained release.

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