scholarly journals OPTIMIZATION OF RIVASTIGMINE CHITOSAN NANOPARTICLES FOR NEURODEGENERATIVE ALZHEIMER; IN VITRO AND EX VIVO CHARACTERIZATIONS

2022 ◽  
pp. 17-27
Author(s):  
MONA IBRAHIM El-ASSAL ◽  
DALIA SAMUEL
Keyword(s):  
Electron Microscopy ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Aqueous Dispersion ◽  
Entrapment Efficiency ◽  
Differential Scanning Calorimetric ◽  
Drug Concentrations

Objective: In an attempt to optimize the anti-Alzheimer effect, rivastigmine-loaded chitosan nanoparticles were developed in order to target of brain through skin permeation. Methods: Rivastigmine-loaded chitosan-tripolyphosphate nanoparticles were prepared by modified ionic gelation method using tween 80 surfactants in different batches with variable chitosan/cross-linker ratios, desirability factors were applied to choose the optimal Nanocarrier and (F15) was selected. Different rivastigmine concentrations were loaded and the highest encapsulation efficiency formulae chosen for further study and evaluated by scanning electron microscopy (SEM), transmission electron microscopy (TEM) and differential scanning calorimetric (DSC). Further, drug loading, Ex-vivo skin permeation of Nano-gel, and kinetic studies were carried out in addition to stability along three months under different temperature. Results: Particle size and polydispersity index showed average 291.6±7.70 to 490.6±7.42 d. nm. and 0.333±0.04 to 0.570±0.023 respectively. The nanoparticles were spherical in shape. Drug concentrations 4% w/w showed the highest drug entrapment efficiency (89.80%) and drug loading (40.81). Ex vivo studies shows that gel formulae of rivastigmine loaded chitosan nanoparticles was not irritant to rat skin had better skin permeation than chitosan nanoparticles aqueous dispersion also capable of releasing the drug in a sustained manner, and follow kinetic diffusion model. Optimum formula F15 was physical and chemical stable. Conclusion: The experimental results showed the suitability of chitosan nanoparticles coated with a surfactant as a potential carrier for permeation through skin and brain, providing sustained delivery of rivastigmine.

scholarly journals DEVELOPMENT, CHARACTERIZATION AND IN VITRO RELEASE KINETIC STUDIES OF IBANDRONATE LOADED CHITOSAN NANOPARTICLES FOR EFFECTIVE MANAGEMENT OF OSTEOPOROSIS

2021 ◽  
pp. 120-125
Author(s):  
S. PATHAK ◽  
S. P. VYAS ◽  
A. PANDEY
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Sodium Tripolyphosphate ◽  
Release Kinetics ◽  
Ph Effect ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR).  Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.

scholarly journals Bioassay-guided optimization of lipid-based erythromycin microparticles

2020 ◽  
Vol 19 (7) ◽  
pp. 1351-1358
Author(s):  
Ifeanyi T. Nzekwe ◽  
Anselm C. Okere ◽  
Ifeanyi E. Okoye ◽  
Kokonne E. Ekere ◽  
Adaobi A. Ezenwa ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Antimicrobial Activities ◽  
Hydrodynamic Size ◽  
Chemical Assay ◽  
Acid Ratio ◽  
Drug Entrapment Efficiency ◽  
Lower Variation

Purpose: To optimize erythromycin microparticles by in vitro bioassay methods based on its antibacterial activity. Methods: The microparticles were produced by high shear homogenization. The effects of different lipid-to-surfactant ratios were studied. The hydrodynamic size of the different batches was evaluated using dynamic light scattering while bioactive drug load per batch was assessed in agar using bioassay methods. The antimicrobial activities of selected batches were tested ex vivo by determination of reduction in bacteraemia following administration of the microparticles to infected animals. Results: All batches had particles with hydrodynamic sizes < 8.5 microns. Batch 7 with a 2: 5: 2.5 (drug: surfactant: stearic acid) ratio, represents the optimized batch with a hydrodynamic size of 2281 nm, a bioactive drug loading capacity (BLC) of 4.67 ± 0.70 % and bioactive drug entrapment  efficiency (BEE) of 10.51 %. The “microparticle MIC” against Staphylococcus aureus was 1.74 x 10-3 μg/ml. Despite containing lower amounts of erythromycin than the pure sample, the microparticles achieved comparable reduction in bacteraemia, with the optimized batch exhibiting lower variation in bacteraemia than the pure drug. Conclusion: Erythromycin microparticles have been successfully optimized with the aid of bioassay methods which has the advantage that only the bioactive drug concentration is factored in. This method eliminates problems posed by inadequate or non-discriminating chemical assay methods. Keywords: Microparticles, Erythromycin, Gastrointestinal, Bioavailability Antimicrobial, Bioactivity, Encapsulation

scholarly journals Effect of cross-linked biodegradable polymers on sustained release of sodium diclofenac-loaded microspheres

2013 ◽  
Vol 49 (4) ◽  
pp. 873-888 ◽  
Author(s):  
Avik Kumar Saha ◽  
Sarbani Dey Ray
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Differential Scanning Calorimetric ◽  
Prolonged Release ◽  
Easy Method ◽  
Calorimetric Analysis ◽  
Sodium Diclofenac

The objective of this study was to formulate an oral sustained release delivery system of sodium diclofenac(DS) based on sodium alginate (SA) as a hydrophilic carrier in combination with chitosan (CH) and sodium carboxymethyl cellulose (SCMC) as drug release modifiers to overcome the drug-related adverse effects and to improve bioavailability. Microspheres of DS were prepared using an easy method of ionotropic gelation. The prepared beads were evaluated for mean particle size, entrapment efficiency, swelling capacity, erosion and in-vitro drug release. They were also subjected to various studies such as Fourier Transform Infra-Red Spectroscopy (FTIR) for drug polymer compatibility, Scanning Electron Microscopy for surface morphology, X-ray Powder Diffraction Analysis (XRD) and Differential Scanning Calorimetric Analysis (DSC) to determine the physical state of the drug in the beads. The addition of SCMC during the preparation of polymeric beads resulted in lower drug loading and prolonged release of the DS. The release profile of batches F5 and F6 showed a maximum drug release of 96.97 ± 0.356% after 8 h, in which drug polymer ratio was decreased. The microspheres of sodium diclofenac with the polymers were formulated successfully. Analysis of the release profiles showed that the data corresponds to the diffusion-controlled mechanism as suggested by Higuchi.

scholarly journals Formulation and Evaluation of Clarithromycin Loaded Nanostructured Lipid Carriers for the Treatment of Acne

2021 ◽  
pp. 26-38
Author(s):  
Pooja Shettigar ◽  
Marina Koland ◽  
S. M. Sindhoor ◽  
Ananth Prabhu
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Acne Treatment

Background: Clarithromycin is a macrolide antibiotic used in acne treatment, but it has poor solubility, which decreases its permeability through lipid barriers such as skin. Nanostructured lipid carriers can enhance the permeability of clarithromycin through the skin, thus improving its potential for controlling acne. Aim: To formulate and evaluate Nanostructured lipid carriers of clarithromycin for topical delivery in acne treatment Methods: Nanostructured lipid carriers were prepared by emulsification and ultrasonication methods using lipids such as glycerol monostearate and oleic with poloxamer 188 as stabilizer. These nano-carriers were optimized with the help of the Quality by Design (QbD) approach employing Design-Expert® software. The nanoparticles were characterized for particle size analysis, zeta potential, drug-excipient compatibility, entrapment efficiency, and surface morphology by Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The nano-carriers were also investigated for in vitro drug release and ex vivo permeation through excised goat skin. The optimized formulation was incorporated into topical carbopol gel base, formulated and examined for pH, viscosity, spreadability, in vitro drug release, ex vivo permeation, and stability under accelerated conditions. Results: The average particle size of the optimized nanoparticles was 164.8 nm, and zeta potential was -39.2 mV. FTIR studies showed that drug and lipids are compatible with each other. The morphology study by SEM and TEM showed spherical shaped particles. The entrapment efficiency of the optimized formulation was found to be 88.16%. In vitro drug release studies indicated sustained release from the formulation due to diffusion through the lipid matrix of the particles. The ex vivo permeation study using goat skin produced greater permeation from the NLC gel (89.5%) than marketed gel (65%) due to the lipid solubility of the nanoparticles in the skin. The formulation was stable under accelerated conditions. Conclusion: The optimized formulation can be considered as promising nano-carriers suitable for the sustained release of clarithromycin into the skin for effective control of acne.

Development and optimization of Luliconazole Nanostructured lipid carriers based gel by Quality by Design its skin distribution studies, dermatokinetic modeling & In-vitro and Ex-vivo correlation

2020 ◽  
Vol 18 ◽  
Author(s):  
Eranti Bhargav ◽  
Yiragamreddy Padmanabha Reddy ◽  
Koteshwara Kunnatur B
Keyword(s):  
Particle Size ◽  
Quality By Design ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Fractional Factorial ◽  
Sonication Time ◽  
Drug Concentrations

Objective : The present study was aimed to improve the permeability of Luliconazole (LZ) and to localize high drug concentrations at skin layers by Quality by Design (QbD) based Nanostructured lipid carriers (NC) based gel. Methods: Quality Target Product Profile was set and Critical Quality attributes were identified. FT-IR and DSC studies confirmed compatibility. Risk assessment was carried out by screening the factors using 27-27-2 fractional factorial design and optimization by Box Behnken design. Cholesterol: Cetyl Palmitate, PEG 200 and probe sonication time were identified as factors, Particle size (<200 nm), PDI (0.4), % Entrapment efficiency (% EE, >80%) and % Cumulative Drug release (% CDR, >95%) as responses. Contour plots, Overlay plots and desirability were utilized to create design space. Results: The quadratic polynomial equations showed that increased lipid content, PEG 200 and optimum sonication time reduced Particle size, PDI, improved % EE and % CDR. The optimized formula was formulated into a gel. Ex-vivo permeation studies performed using pig ear pinna skin revealed that developed LZ NC gel exhibited greater permeation 272.98±8.57 (µg/cm2 ) and 32.11 ±4.7 (µg/cm2 /h) flux than plain drug dispersed gel. Dermatokinetic parameters of LZ NC gel revealed that highly significant amount of LZ was permeated, distributed and transported through the skin layers. The better linear correlations were obtained by LZ permeation through synthetic membrane (in-vitro) and pig ear pinna skin (ex-vivo). Conclusion: The above findings revealed that developed LZ NC gel exhibited better permeation and localization at skin layers in treating fungal infections.

Preparation of Chitosan Nanoparticles for Protein Delivery by w/o/w Emulsion Solvent Evaporation and Simple Ionotropic Gelation Techniques

2007 ◽  
Vol 121-123 ◽  
pp. 751-754 ◽  
Author(s):  
Garnpimol C. Ritthidej ◽  
W. Pichayakorn ◽  
Chulalongkorn Kusonwiriyawong ◽  
V. Lipipun
Keyword(s):  
Protein Delivery ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Form Complex ◽  
Ionotropic Gelation

The purpose of this study was to prepare chitosan nanoparticles (CS NP) for controlled protein delivery. Two techniques, simple ionotropic gelation (method [I]) and w/o/w emulsion solvent evaporation containing ionotropic gelation (method [II]), were used to prepare CS NP. Tripolyphosphate (TPP) and Eudragit L100-55 (Eud) were used as anionic agents to form complex with cationic chitosan. Bovine serum albumin (BSA) was encapsulated into NP. The morphological characteristics, particle size and size distribution, protein entrapment efficiency, zeta potential, in vitro release, protein secondary structure and its integrity were investigated. The results showed that CS NP could be prepared by appropriate cationic and anionic ratios in both methods. Excess anionic agents resulted in particle aggregation of micron size. The median sizes of particles were between 0.127-0.273 mcm with method [I] provided the smallest size. The 0.02-0.10% BSA loaded preparations showed the same particle sizes and size distributions as blank preparations. SEM photomicrographs revealed that the obtained NP were spherical. Protein entrapment efficiency was between 47-84% and increased when decreasing the percentage of drug loading. The method [II] with TPP exhibited the highest protein entrapment efficiency, following by the method [II] with Eud and method [I] with TPP, respectively. The zeta potentials were positive. Prolonged in vitro protein release profiles were observed from all preparations of CS NP. After 10 days, the release was between 53-72%. Circular dichroism and SDS-polyaceylamide gel electrophoresis techniques confirmed that these processes did not have any destructive effect on the protein structure. Therefore these preparation techniques could be used to encapsulate water-soluble drugs, proteins, DNA, or antigens into CS NP as effective delivery carriers.

scholarly journals Topical Delivery of Apremilast Loaded Nanostructured Lipid Carrier Based Hydrogel for Psoriasis Therapy

2021 ◽  
pp. 7-20
Author(s):  
S. M. Sindhoor ◽  
Marina Koland
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Extended Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Transmission Electron ◽  
Psoriasis Therapy ◽  
Systemic Side Effects

Background: Apremilast (APR) is an orally administered selective phosphodiesterase 4 inhibitor approved to treat plaque psoriasis and psoriatic arthritis and is available as an oral tablet formulation. However, its systemic side effects limit its application. The low solubility and permeability of apremilast make it difficult to administer it through the skin. Hence an attempt is made to incorporate apremilast into a suitable nanocarrier to facilitate its topical delivery. Aims: To formulate and characterize Apremilast loaded nanostructured lipid carriers for the management of psoriasis to reduce the systemic side effects. Methodology: Apremilast loaded Nanostructured Lipid carriers (NLC) were prepared by melt emulsification accompanied by probe sonication. The formulation was prepared using GMS, Sefsol 218, Tween 80 and Transcutol P as Solid Lipid, Liquid lipid, Surfactant and Penetration Enhancer. The NLC was incorporated into carbapol 934 dispersion to convert it into a gel. The NLC formulation was evaluated for size, Polydispersity Index, Zeta Potential, Entrapment efficiency,  Transmission Electron Microscopy. After that, the NLC gel was examined for Spreadability, Extrudabilty, Viscosity, In vitro drug release, Ex vivo permeation, Skin deposition and In vivo studies. Results: The formulated Apremilast loaded showed particle size of less than 200 nm (i.e.170.32nm) with a narrow PDI of 0.267. Entrapment efficiency revealed that 89.26±01.22% of the drug was entrapped. Transmission electron microscopy images confirmed the spherical nature of the nanocarrier. The extended-release pattern of the formulated NLC for 24h was observed in the in vitro release studies and followed the Higuchi model(R2=0.9966). Ex vivo permeability showed a 6.14 fold increase in permeability and 74.05±0.25% deposition of apremilast loaded NLC gel compared to apremilast gel. The formulation was stable for three months without significant changes. In vivo skin studies showed that the prepared NLC did not have any skin irritation potential. The antipsoriatic activity demonstrated by the Apremilast loaded NLC gel in the imiquimod induced psoriasis model in mice was comparable to the standard treatment. Conclusion: Apremilast loaded NLC demonstrated enhanced permeation, improved skin retention and extended-release compared to conventional gel. The developed formulation can be an alternative for psoriasis therapy after clinical trials in the future.

scholarly journals CIPROFLOXACIN HYDROCHLORIDE LOADED CHITOSAN NANOPARTICLE GEL: ADVANCED APPROACH FOR ENHANCING PERMEATION AND SUSTAINABILITY OF DRUG RELEASE

2018 ◽  
Vol 6 (4) ◽  
pp. 67-72
Author(s):  
Dhruv Dev ◽  
Urvashi Bhardwaj ◽  
D N Prasad
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Ciprofloxacin Hydrochloride ◽  
Zero Order Kinetics ◽  
In Vitro Permeation ◽  
Chitosan Nanoparticle ◽  
Dsc Method

Transdermal drug delivery is one of the most reliable, appealing and effective technique which provides controlled and constant administration of drug. The aim of the study was to develop a gel form of nanoparticles loaded with ciprofloxacin hydrochloride in order to enhance the permeability of drug and for the release of drug over a period of 24 hrs. The nanoparticles were formulated by ionic gelation method using chitosan as a polymer and TPP as a cross linking agent. The compatibility of drug and polymer is studied by using FTIR spectroscopy and DSC method. There was no interaction observed by UV and FTIR study. The six different batches were prepared using different polymer and drug ratio. The fourth batch (N4) shows best results as compared to others which was used for further investigations. The formulation was then optimized for its particle size, zeta potential, morphology, drug content, drug entrapment efficiency, drug loading capacity and in-vitro permeation. TEM study reveals that the nanoparticles are spherical in shape and also confirms the size below 500nm. Drug release studies shows that nanoparticles could release drug for 24 hrs and follows zero order kinetics. From DSC analysis it was found that the drug was effectively encapsulated inside the chitosan nanoparticles. Finally, it was concluded that the penetration of ciprofloxacin hydrochloride was enhanced after loading it into chitosan nanoparticles and also the drug was release over 24 hrs.   Keywords: Nanoparticles, Ciprofloxacin Hydrochloride, Chitosan, Carbopol 934

scholarly journals Formulation and In-Vitro Characterization of Chitosan-Nanoparticles Loaded with the Iron Chelator Deferoxamine Mesylate (DFO)

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 238 ◽  
Author(s):  
Maria Lazaridou ◽  
Evi Christodoulou ◽  
Maria Nerantzaki ◽  
Margaritis Kostoglou ◽  
Dimitra Lambropoulou ◽  
...  
Keyword(s):  
Sodium Tripolyphosphate ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Release Mechanism ◽  
Hydroxyl Groups ◽  
Deferoxamine Mesylate ◽  
Pharmacologically Active

The objective of this study was to develop chitosan (CS) nanoparticles (NPs) loaded with deferoxamine mesylate (DFO) for slow release of this iron-chelating drug. Drug nanoencapsulation was performed via ionic gelation of chitosan using sodium tripolyphosphate (TPP) as cross-linker. Nanoparticles with a size ranging between 150 and 400 nm were prepared for neat CS/TPP with a 2/1 molar ratio while their yield was directly dependent on the applied stirring rate during the preparation process. DFO at different content (20, 45 and 75 wt %) was encapsulated into these nanoparticles. We found that drug loading correlates with increasing DFO content while the entrapment efficiency has an opposite behavior due to the high solubility of DFO. Hydrogen-bonding between amino and hydroxyl groups of DFO with reactive groups of CS were detected using FT-IR spectroscopy while X-ray diffraction revealed that DFO was entrapped in amorphous form in the CS nanoparticles. DFO release is directly dependent on the content of loaded drug, while model analysis revealed that the release mechanism of DFO for the CS/TPP nanoparticles is by diffusion. Treatment of murine RAW 264.7 macrophages with nanoencapsulated DFO promoted an increased expression of transferrin receptor 1 (TfR1) mRNA, a typical homeostatic response to iron deficiency. These data provide preliminary evidence for release of pharmacologically active DFO from the chitosan nanoparticles.

scholarly journals FORMULATION AND OPTIMIZATION OF QUERCETIN LOADED NANOSPONGES TOPICAL GEL: EX VIVO, PHARMACODYNAMIC AND PHARMACOKINETIC STUDIES

2019 ◽  
pp. 156-165
Author(s):  
Y. SARAH SUJITHA ◽  
Y. INDIRA MUZIB
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Diffusion Method ◽  
Pharmacokinetic Studies ◽  
Topical Gel

Objective: Quercetin is therapeutically hampered because of its poor solubility. The present investigation was aimed to prepare quercetin loaded nanosponges topical gel to enhance the solubility and efficacy of the drug. Methods: Quercetin nanosponges were prepared by emulsion solvent diffusion method. Developed nanosponges optimized by particle size, SEM, entrapment efficiency, FT-IR, DSC, P-XRD, In vitro studies. The optimized formulation of nanosponges was loaded into a topical gel and it was characterized by ex-vivo, in vivo Pharmacodynamic and kinetic studies. Results: The particle size and zeta potential of optimized nanosponges were found to be 188.3 nm and-0.1mV. Surface morphology was studied using SEM Analysis which showed tiny sponge-like structure and entrapment efficiency was found to be 96.5 %. In vitro drug release of optimized nanosponges was found to be 98.6% for 7hours. Optimized nanosponges entrapped gel was prepared by using carbopol 934 and hydroxypropyl methylcellulose as gelling agents. The prepared nanogels were homogenous and ex-vivo skin permeation studies of the optimized nanosponges gel was found to be 98.1% for 5 h, quercetin loaded nanosponges has shown higher skin permeation efficiency (18.4µg/cm2±2.1) compared to pure quercetin gel. The pharmacokinetic and pharmacodynamic studies showed that the quercetin loaded nanosponges has shown more effective when compared to marketed formulation. Conclusion: Quercetin loaded nanosponges gel has shown a significant increase in activity (p<0.05) compared to the marketed formulation (Voveran Emulgel).

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