scholarly journals PLGA NANOPARTICLES LOADED MUCOADHESIVE AND THERMOSENSITIVE HYDROGEL AS A POTENTIAL PLATFORM FOR THE TREATMENT OF ORAL MUCOSITIS

2019 ◽  
Vol 11 (1) ◽  
pp. 106
Author(s):  
Gina S. El-feky ◽  
Gamal M. Zayed
Keyword(s):  
Oral Mucositis ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Plga Nanoparticles ◽  
Complete Healing ◽  
Drug Release Profile ◽  
Thermosensitive Hydrogel ◽  
Hydrogel Matrix

Objective: The objective of this study was to design an effective topical treatment for oral mucositis.Methods: Poly-(DL-lactide-co-glycolide) (PLGA) nanoparticles (NPs) and Poloxamer407 (PLX)/Hydroxy propyl methyl cellulose (HPMC) hydrogel matrix (HG) were used as combined carriers for benzydamine HCL (BNZ). BNZ loaded PLGA nanoparticles were assessed for their particle size, PDI, zeta potential and entrapment efficiency. Scanning electron microscopy, thermosensitivity study, mucoadhesion study, in vitro release and in vivo investigation were used to characterize the combined BZN loaded PLGA NPs HG.Results: Negatively charged NPs with an average diameter of 139±4.92 nm were incorporated into PLX/HPMC HG bases. The gelation temperature of BZN-PLGA-NPs-HGs ranged between 31°C and 36.5°C. When diluted with saliva simulated fluid, BZN-PLGA-NPs-HGs preserved their gelation properties. Mucoadhesion was found lower for formulations prepared with PLX without HPMC. An increase in the concentrations of PLX from 10 to 30% resulted in an increase in adhesion. Both PLGA-NPs and PLGA-NPs-HG provided a biphasic drug release profile while BZN-HG provided monophasic zero order release pattern. The in vivo study showed that animal groups treated with BZN-HG and BZN-PLGA-NPs-HG showed a significantly higher reduction percentage in ulcer surface area compared to those treated with BZN-PLGA-NPs. BZN-PLGA-NPs-HG group needed 10 d of treatment to complete healing versus 16 d, 14 d and 12 d for the complete healing of groups with no treatment, treated with BZN-PLGA-NPs and treated with BZN-HG, respectively.Conclusion: BZN-PLGA-NPs-HG could represent a promising mean for the effective treatment of oral mucositis induced by cancer therapy.

Formulation and Evaluation of Atorvastatin Calcium-Poly-ε-Caprolactone Nanoparticles Loaded Ocular Inserts for Sustained Release and Antiinflammatory Efficacy

2020 ◽  
Vol 21 (15) ◽  
pp. 1688-1698
Author(s):  
Germeen N.S. Girgis
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Average Weight ◽  
Drug Release Profile ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Purpose: The work was performed to investigate the feasibility of preparing ocular inserts loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system. Methods: First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with free drug-loaded ocuserts. Results: The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and 62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to 0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability, ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant lowering in PMN count after 3h. Conclusion: These findings proposed a possibly simple, new and affordable price technique to prepare promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory efficacy.

scholarly journals Development of a Topical Insulin Polymeric Nanoformulation for Skin Burn Regeneration: An Experimental Approach

2021 ◽  
Vol 22 (8) ◽  
pp. 4087
Author(s):  
Maria Quitério ◽  
Sandra Simões ◽  
Andreia Ascenso ◽  
Manuela Carvalheiro ◽  
Ana Paula Leandro ◽  
...  
Keyword(s):  
Wound Healing ◽  
Healing Process ◽  
In Vitro Release ◽  
Peptide Hormone ◽  
Plga Nanoparticles ◽  
Wound Healing Process ◽  
Target Area ◽  
Encapsulation Process

Insulin is a peptide hormone with many physiological functions, besides its use in diabetes treatment. An important role of insulin is related to the wound healing process—however, insulin itself is too sensitive to the external environment requiring the protective of a nanocarrier. Polymer-based nanoparticles can protect, deliver, and retain the protein in the target area. This study aims to produce and characterize a topical treatment for wound healing consisting of insulin-loaded poly-DL-lactide/glycolide (PLGA) nanoparticles. Insulin-loaded nanoparticles present a mean size of approximately 500 nm and neutral surface charge. Spherical shaped nanoparticles are observed by scanning electron microscopy and confirmed by atomic force microscopy. SDS-PAGE and circular dichroism analysis demonstrated that insulin preserved its integrity and secondary structure after the encapsulation process. In vitro release studies suggested a controlled release profile. Safety of the formulation was confirmed using cell lines, and cell viability was concentration and time-dependent. Preliminary safety in vivo assays also revealed promising results.

COMPARATIVE EVALUATION OF POLYMER COMBINATION IN THE DESIGN OF BRIMONIDINE TARTRATE OCULAR INSERTS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (07) ◽  
pp. 30-35
Author(s):  
P Goudanavar ◽  
◽  
N Ambhore ◽  
D. Hiremath ◽  
R Udupi
Keyword(s):  
Polymer Concentration ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Carboxymethyl Chitosan ◽  
Moisture Loss ◽  
In Vivo Release ◽  
Weight Variation ◽  
Brimonidine Tartrate

Brimonidine is an anti-glaucoma agent useful in treatment of intraocular pressure. In the present study an attempt was made to formulate ophthalmic inserts of brimonidine tartrate (BT) in combination with polymers like methylcellulose, carboxymethyl chitosan and HPMC. Prepared ocular films were evaluated for uniformity in thickness, weight variation, % moisture absorption, % moisture loss, in vitro and in vivo release studies. The physical characteristics of the films were found to be within acceptable limits. The study confirmed that brimonidine tartrate can be delivered through films made of methyl cellulose, carboxymethyl chitosan and HPMC combination matrix cast with ethyl cellulose (EC). In vitro release study revealed that increasing the proportion of polymer concentration decreased the rate of release of brimonidine tartrate. In vivo release profile of ocular inserts revealed controlled release of drug over a period of 24 h. Optimized formulation CH3 was evaluated for in vivo release characteristics using rabbits as animal model. The optimized formulation CH3 was found to be stable at accelerated storage condition of 40/75 % RH.

scholarly journals A Mixed Thermosensitive Hydrogel System for Sustained Delivery of Tacrolimus for Immunosuppressive Therapy

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 413 ◽  
Author(s):  
Hsiu-Chao Lin ◽  
Madonna Rica Anggelia ◽  
Chih-Chi Cheng ◽  
Kuan-Lin Ku ◽  
Hui-Yun Cheng ◽  
...  
Keyword(s):  
Immunosuppressive Therapy ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Immunosuppressive Agent ◽  
Sustained Delivery ◽  
Thermosensitive Hydrogel ◽  
Thermosensitive Hydrogels ◽  
Hydrogel System

Tacrolimus is an immunosuppressive agent for acute rejection after allotransplantation. However, the low aqueous solubility of tacrolimus poses difficulties in formulating an injection dosage. Polypeptide thermosensitive hydrogels can maintain a sustained release depot to deliver tacrolimus. The copolymers, which consist of poloxamer and poly(l-alanine) with l-lysine segments at both ends (P–Lys–Ala–PLX), are able to carry tacrolimus in an in situ gelled form with acceptable biocompatibility, biodegradability, and low gelling concentrations from 3 to 7 wt %. By adding Pluronic F-127 to formulate a mixed hydrogel system, the drug release rate can be adjusted to maintain suitable drug levels in animals with transplants. Under this formulation, the in vitro release of tacrolimus was stable for more than 100 days, while in vivo release of tacrolimus in mouse model showed that rejection from skin allotransplantation was prevented for at least three weeks with one single administration. Using these mixed hydrogel systems for sustaining delivery of tacrolimus demonstrates advancement in immunosuppressive therapy.

scholarly journals FABRICATION OF BIOADHESIVE OCUSERT WITH DIFFERENT POLYMERS: ONCE A DAY DOSE

2018 ◽  
Vol 10 (6) ◽  
pp. 309
Author(s):  
Aya M. Dawaba ◽  
Hamdy M. Dawaba ◽  
Amal S. M. Abu El-enin ◽  
Maha K. A. Khalifa
Keyword(s):  
In Vitro Release ◽  
Methyl Cellulose ◽  
Storage Period ◽  
Poly Vinyl Alcohol ◽  
Release Kinetic ◽  
Casting Technique ◽  
Process Characterization ◽  
Vitro Release

Objective: The objective of this current study is to fabricate ocuserts to control the drug release from chosen bioadhesive polymeric matrixes to enhance patient compliance. Ciprofloxacin HCl (CFX HCl) was selected as a model drug.Methods: Different bioadhesive polymers with different film forming capabilities namely Hydroxy Propyl Methyl Cellulose (HPMC K4M), Poly Vinyl Alcohol (PVA), Sodium Carboxy Methyl Cellulose (Na CMC), Hydroxy Propyl Cellulose (HPC), Sodium Alginate (Na Alg.), pullulan and Xanthan Gum (XG) in different ratios were used in fabricating ocuserts using solvent-casting technique. Propylene Glycol (PG) was used as a plasticizer to facilitate the fabrication process. Characterization tests of the developed ocuserts were performed as well as bioadhesive tests and in vitro release studies of the incorporated drug. The obtained results were analysed using different release kinetic models. Stability of the selected ocuserts was investigated at 40±0.5 °C and 75±5% Relative Humidity (RH) for three months’ storage period. In vivo ocular irritation test was performed to investigate the safety of the formula in rabbits’ eyes as well as to test the release profile and thus to estimate In vitro In vivo correlation.Results: All the prepared ocuserts showed the uniformity of film characterization and bioadhesion strength ranged from 240±66 and 158±52dyne/cm2. Selected formula from the in vitro release study tested for in vivo study showed the slow release of ciprofloxacin drug up to 24 h with no signs of eye irritancy. Results for In vitro In vivo correlation showed an excellent correlation with R2 value of 0.9982.Conclusion: PVA based ocuserts proven to be a promising once-daily, effective and safe ocular delivery system of the drug.

A mucoadhesive thermosensitive hydrogel containing erythropoietin as a potential treatment in oral mucositis: in vitro and in vivo studies

2018 ◽  
Vol 8 (5) ◽  
pp. 1226-1237 ◽  
Author(s):  
Mahboubeh Rezazadeh ◽  
Niloofar Jafari ◽  
Vajihe Akbari ◽  
Marjan Amirian ◽  
Majid Tabbakhian ◽  
...  
Keyword(s):  
Oral Mucositis ◽  
In Vivo Studies ◽  
Potential Treatment ◽  
Thermosensitive Hydrogel

scholarly journals Ligand Decorated Embelin Loaded PLGA Nanoparticles for Management of Alcohol Induced Hepatotoxicity

2020 ◽  
Vol 10 (1) ◽  
pp. 72-80
Author(s):  
Ajay Kumar ◽  
M. Nikhat Khan ◽  
Jovita Kanoujia ◽  
Amandeep Singh ◽  
Neeraj Mishra
Keyword(s):  
High Performance ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Hep G2 ◽  
Release Studies ◽  
Plga Nanoparticle ◽  
Surface Modified ◽  
Vitro Release

Preparation of surface modified Embelin loaded nanoparticles (GA-PEG-PLGA) for the management of hepatotoxicity. Surface modified Embelin loaded GA-PEG-PLGA NPs were evaluated by NMR, FTIR, TEM techniques and in vitro release studies. The biodistribution of the nanoparticles was assessed by High-performance liquid chromatography (HPLC), and the cellular uptake study was evaluated using Hep G2 cells (liver cells lines). The hepatoprotecttive effect of the surface modified Embelin loaded GA-PEG-PLGA NPs was investigated in-vitro and in-vivo. The surface modified Embelin loaded GA-PEG-PLGA nanoparticles significantly increases the uptake of drug in liver by 2.5 folds more than plain drug. Keywords: Glycyrrhetinic acid, Receptor mediated, Surface functionalization, Embelin, PLGA nanoparticle.

Development and In vivo Bioavailability Evaluation of Sumatriptan Succinate Buccal Tablets

2014 ◽  
Vol 7 (2) ◽  
pp. 2477-2486
Author(s):  
Sudarshan Singh ◽  
Dharmesh Savaliya ◽  
Suresh Shah D. ◽  
Sunil Bothara B
Keyword(s):  
Ex Vivo ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Compatibility Study ◽  
Surface Ph ◽  
Sumatriptan Succinate ◽  
Buccal Tablets

In the present investigation an attempt has made to design mucoadhesive buccal tablets of sumatriptan succinate to improve its bioavailability. The mucoadhesive buccal tablets were prepared by wet granulation procedure using different concentration of polycarbophil and hydroxy propyl methyl cellulose K4M alone. Compatibility study of drug and polymer were performed by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Precompression property of sumatriptan succinate was evaluated to check the suitability of compression method. Postcompressional parameters such as weight variation, hardness, thickness, surface pH, in vitro drug release, ex vivo bioadhesion time, ex vivo mucoadhesive strength, ex vivo permeation study and in vivo bioavailability study of optimized formulation were evaluated. FTIR spectroscopy and DSC study revealed that there was no possible interaction between drug and polymers, because no major change in peaks were obtained. The precompression parameters were in acceptable range of pharmacopoeial specification. The surface pH of the tablets was in the range of salivary pH (6.5 to 7.5) and tablets showed good ex vivo bioadhesion time up to 10 hr which indicated good adhesive capacity of tablets. The in vitro release of optimized formulation obeyed zero order kinetics with non-Fickian anomalous diffusion mechanism. The percentage relative bioavailability of sumatriptan succinate from optimized buccal tablets was found to be 152.76 %. Buccal tablets of sumatriptan succinate were successfully prepared with improved bioavailability.

scholarly journals RADITYA ISWANDANA, KURNIA SARI SETIO PUTRI, RANDIKA DWIPUTRA, TRYAS YANUARI, SANTI PURNA SARI, JOSHITA DJAJADISASTRA

2017 ◽  
Vol 9 (5) ◽  
pp. 109
Author(s):  
Raditya Iswandana ◽  
Kurnia Sari Setio Putri ◽  
Randika Dwiputra ◽  
Tryas Yanuari ◽  
Santi Purna Sari ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Tripolyphosphate ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Process Efficiency ◽  
Drug Release Profile ◽  
Eudragit L100

Objective: Drug delivery to the colon via oral route can be directly treated a variety of diseases in the colon, such as fibrosis. Tetrandrine is a drug that has anti-fibrosis effects. In this study, chitosan-tripolyphosphate (TPP) beads containing tetrandrine was made and evaluated for in vitro release profile and in vivo targeted test.Methods: Chitosan-TPP tetrandrine beads were prepared by ionic gelation method with variation in sodium tripolyphosphate concentration: 3% (Formula 1), 4% (Formula 2), and 5% (Formula 3). All formulae were characterized for its morphology, particle size, moisture content, process efficiency, entrapment efficiency, thermal character, crystallinity, and swelling. Then, the best formula was coated with HPMCP HP-55, CAP, Eudragit L100-55, or Eudragit L100 prior to drug release profile in vitro and in vivo test.Results: Beads from all formulae had an average size: 920.50±0.04 µm, 942.21±0.08 µm, and 1085.95±0.03 µm; Water content: 7.28±0.003%, 5.64±0.005%, and 6.84±0.004%; Process efficiency: 29.70%, 28.96%, and 29.70%; Entrapment efficiency: 16.20±0.63%, 17.02±0.37%, and 20.42±0.70% for Formula 1, 2, and 3, respectively. In addition, the results of in vitro cumulative drug release were 67.36%, 76.04%, 83.12%, 83.21%, 40.16%, 37.98%, 45.86%, 41.71% for Formula 3A-3H, respectively.Conclusion: It can be concluded that Formula 3D (CAP 15%) was chosen as a formulation with the best in vitro profile. Moreover, the in vivo targeted test showed that Formula 3D was able to deliver the beads to the intestine compared to the control beads.

scholarly journals Effect of Dexamethasone-Loaded PLGA Nanoparticles on Oral Mucositis Induced by 5-Fluorouracil

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 53
Author(s):  
Susana Barbosa Ribeiro ◽  
Aurigena Antunes de Araújo ◽  
Maisie Mitchele Barbosa Oliveira ◽  
Alaine Maria dos Santos Silva ◽  
Arnóbio Antônio da Silva-Júnior ◽  
...  
Keyword(s):  
Oral Mucositis ◽  
Hematopoietic Cell Transplantation ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Mechanical Trauma ◽  
Tnf Α ◽  
Cox 2 ◽  
Emulsification Solvent Evaporation ◽  
Almost All

Oral mucositis (OM) is characterized by the presence of severe ulcers in the oral region that affects patients treated with chemotherapy. It occurs in almost all patients who receive radiotherapy of the head and neck, as well as patients who undergo hematopoietic cell transplantation. The pathophysiology of OM is complex, and there is no effective therapy. The aim of this study was to evaluate the effect of dexamethasone-loaded poly(d,l-Lactic-co-glycolic) nanoparticles (PLGA-DEX NPs) on an OM model induced in hamsters. The NPs were synthesized using the emulsification-solvent evaporation method and were characterized by the size, zeta potential, encapsulation efficiency, atomic force microscopy, physicochemical stability, and the in vitro release. The OM was induced by the administration of 5-FU on the first and second days and mechanical trauma on the 4th day of the experiment. PLGA-DEX NPs were administered to treat OM. The animals were euthanized on the 10th day. Macroscopic and histopathological analyses were performed, measurement of malonaldehyde (MDA) and ELISA was used to determine the levels of IL-1β and TNF-α. Immunoexpressions of NF-κB, COX-2, and TGF-β were determined by immunohistochemistry, and qRT-PCR was used to quantify the gene expression of the GILZ, MKP1, and NF-κB p65. The PLGA-DEX NPs (0.1 mg/kg) significantly reduced macroscopic and histopathological scores, decreased MDA, TNF-α and IL-1β levels, immunostaining for NF-κB, COX-2, TGF-β, and suppressed NF-κB p65 mRNA expression, but increased GILZ and MKP1 expression.

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