scholarly journals Modulation of Entrapment Efficiency and In Vitro Release Properties of BSA-Loaded Chitosan Microparticles Cross-Linked with Citric Acid as a Potential Protein–Drug Delivery System

Materials ◽  
2020 ◽  
Vol 13 (8) ◽  
pp. 1989 ◽  
Author(s):  
Natalia Sedyakina ◽  
Andrey Kuskov ◽  
Kelly Velonia ◽  
Nataliya Feldman ◽  
Sergey Lutsenko ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Citric Acid ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Release Mechanism ◽  
Model Protein ◽  
Cross Linker ◽  
The Cross

Microparticles, aimed for oral protein and peptide drug delivery, were prepared via emulsion cross-linking using citric acid as cross-linker and polyglycerol polyricinoleate as surfactant. A comparative study of the interaction between chitosan and citric acid and its effect on the resulting microparticle properties was performed using different chitosan-to-cross-linker mass ratios and pH-values during fabrication of the microparticles. Non-cross-linked and cross-linked microparticles were studied in terms of size (4–12 μm), zeta potential (−15.7 to 12.8 mV), erosion (39.7–75.6%), a model protein encapsulation efficiency (bovine serum albumin) (6.8–27.6%), and loading capacity (10.4–40%). Fourier transform infrared spectroscopy and X-ray diffraction confirmed the ionic interaction between the protonated amine groups of chitosan and the carboxylate ions of the cross-linking agent. Scanning electron microscopy revealed that the non-cross-linked microparticles had an uneven shape with wrinkled surfaces, while the cross-linked formulations were spherical in shape with smooth surfaces. On the basis of these data, the role of the surfactant and microparticle structure on the release mechanism was proposed. Control of the microparticle shape and release mechanisms is expected to be crucial in developing carriers for the controlled delivery of proteins and peptides.

Effect of Surfactants on Characteristic and In Vitro Release of Meloxicam Loaded in Deformable Liposomes

2012 ◽  
Vol 506 ◽  
pp. 457-460
Author(s):  
Sureewan Duangjit ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Drug Delivery ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sodium Cholate ◽  
Drug Delivery Carrier ◽  
Release Study ◽  
Water Insoluble Drug ◽  
Vitro Release ◽  
Potential Use

The aim of this study was to investigate the effect of surfactants on characteristic and in vitro release of liposomes containing meloxicam (MX), model of water insoluble drug. The potential use of deformable liposomes for drug delivery system was developed and investigated. The formulation composed of constant amount of phosphatidylcholine (PC) and MX and various amounts of cholesterol (Chol), sodium cholate (NaChol), sodium oleate (NaO) and stearylamine (SA) was formulated by reverse phase evaporation method. The vesicle size, zeta potential, morphology, entrapment efficiency, loading efficiency, stability andin vitrorelease study were evaluated. The result indicated that the entrapment efficiency andin vitrorelease study of vesicle formulations containing surfactants were significantly higher than the conventional liposome and MX suspension. The formulation of 10:2:2:5 PC/MX/Chol/NaO provided the maximum entrapment efficiency and drug release. Our research suggested that MX loaded in deformable liposomes containing surfactants can be potentially used as a drug delivery carrier for water insoluble drug.

Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhaskar Kurangi ◽  
Sunil Jalalpure ◽  
Satveer Jagwani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Topical Application ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF DOXORUBICIN LOADED SOLID LIPID NANOSUSPENSION FOR NOSE TO BRAIN DELIVERY USING DESIGN EXPERT SOFTWARE

2021 ◽  
pp. 45-57
Author(s):  
VIRAG A. SHAH ◽  
JAYVADAN K. PATEL
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
High Speed ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Brain Targeting ◽  
Solid Lipid ◽  
Stirring Time

Objective: The goal of the current study was to investigate the possible use of solid lipid nanosuspension (SLNs) as a drug delivery method to boost doxorubicin (DOX) brain-targeting performance after intranasal (i. n.) administration.  Methods: 33 factorial design was applied for optimization by using lipid concentration, surfactant concentration, and High-speed homogenizer (HSH) stirring time as dependent variables, and their effect was observed on particles size, Polydispersity index (PDI), and entrapment efficiency.  Results: With the composition of Compritol® 888 ATO (4.6 % w/v), tween 80 (1.9 % w/v), and HSH stirring time, the optimized formula DOX-SLNs prepared (10 min). Particle size, PDI, zeta potential, entrapment efficiency, percent in vitro release were found to be 167.47±6.09 nm, 0.23±0.02, 24.1 mV, 75.3±2.79, and 89.35±3.27 percent in 24 h, respectively, for optimized formulation (V-O). No major changes in particle size, zeta potential, and entrapping efficiency were found in the stability studies at 4±2 °C (refrigerator) and 25±2 °C/60±5% RH up to 3 mo.  Conclusion: Following the non-invasive nose-to-brain drug delivery, which is a promising therapeutic strategy, the positive findings confirmed the current optimized DOX-loaded SLNs formulation.

scholarly journals HESPERIDIN HYDROGEL FORMULATION USING PECTIN-CHITOSAN POLYMER COMBINATION

2017 ◽  
Vol 9 (12) ◽  
pp. 98 ◽  
Author(s):  
Andhi Fahrurroji ◽  
Dea Thendriani ◽  
Hafrizal Riza
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
The Body ◽  
Flavonoid Glycosides ◽  
Release Mechanism ◽  
Factorial Method ◽  
Optimum Formula ◽  
Therapy Target

Objective: Hesperidin is flavonoid glycosides that proven to have therapeutic activity to any desease, one of them is colon disease; but, its low solubility (< 100 mg/L) makes small absosption inside the body so it needs delivery system that could deliver hesperidin to the therapy target. The objective of this research is to get optimum formula from hydrogel with polimer pectin-chitosan combination that can control in vitro hesperidin release.Method: Optimum hydrogel formula determination using Design Expert 7.0.0 with factorial method design, resulted in formula plans with pectin-chitosan consentration comparison of (P3% : C1%), (P3% : C2%), (P5% : C1%), (P5% : C2%) respectively.Result: Optimum formula with pectin : chitosan concentration comparison (5% : 1%) has entrapment efficiency about 96.658%; k(/hour) swelling index at pH 5.0, 6.8, and 7.4, about 34.917, 15.766, and 8.146 respectively; drug release at pH 5.0, 6.8, and a medium contained 2% mouse’s caecum  about 0.461, 20.116, and 52.955% respectively; and the mucoadhesive strength about 0.184 N/cm2.Conclusion: The combination of pectin-chitosan polymer in hydrogel muchoadhesive matrix can control hesperidin in vitro release with the drug release value at the highest concentration of pectin in medium contained 2% mouse’s saecum that could release drug about 56%. Hesperidin hydrogel release mechanism follows Higuchi kinetic.

scholarly journals Nanostructured Lipid Carriers to Mediate Brain Delivery of Temazepam: Design and In Vivo Study

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 451 ◽  
Author(s):  
Nermin E. Eleraky ◽  
Mahmoud M. Omar ◽  
Hemat A. Mahmoud ◽  
Heba A. Abou-Taleb
Keyword(s):  
Drug Delivery ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Relative Bioavailability ◽  
Nanostructured Lipid Carriers ◽  
Brain Targeting ◽  
Pharmacokinetic Data ◽  
Average Size

The opposing effect of the blood–brain barrier against the delivery of most drugs warrants the need for an efficient brain targeted drug delivery system for the successful management of neurological disorders. Temazepam-loaded nanostructured lipid carriers (NLCs) have shown possibilities for enhancing bioavailability and brain targeting affinity after oral administration. This study aimed to investigate these properties for insomnia treatment. Temazepam-NLCs were prepared by the solvent injection method and optimized using a 42 full factorial design. The optimum formulation (NLC-1) consisted of; Compritol® 888 ATO (75 mg), oleic acid (25 mg), and Poloxamer® 407 (0.3 g), with an entrapment efficiency of 75.2 ± 0.1%. The average size, zeta potential, and polydispersity index were determined to be 306.6 ± 49.6 nm, −10.2 ± 0.3 mV, and 0.09 ± 0.10, respectively. Moreover, an in vitro release study showed that the optimized temazepam NLC-1 formulation had a sustained release profile. Scintigraphy images showed evident improvement in brain uptake for the oral 99mTc-temazepam NLC-1 formulation versus the 99mTc-temazepam suspension. Pharmacokinetic data revealed a significant increase in the relative bioavailability of 99mTc-temazepam NLC-1 formulation (292.7%), compared to that of oral 99mTc-temazepam suspension. Besides, the NLC formulation exhibited a distinct targeting affinity to rat brain. In conclusion, our results indicate that the developed temazepam NLC formulation can be considered as a potential nanocarrier for brain-mediated drug delivery in the out-patient management of insomnia.

scholarly journals Modified Carboxyl-Terminated PAMAM Dendrimers as Great Cytocompatible Nano-Based Drug Delivery System

2019 ◽  
Vol 20 (8) ◽  
pp. 2016 ◽  
Author(s):  
Minh Thanh Vu ◽  
Long Giang Bach ◽  
Duy Chinh Nguyen ◽  
Minh Nhat Ho ◽  
Ngoc Hoi Nguyen ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Malignant Cell ◽  
Pamam Dendrimers ◽  
Optimal Size

Polyamidoamine (PAMAM) dendrimers are extensively researched as potential drug delivery system thanks to their desirable features such as controlled and stable structures, and ease of functionalization onto their surface active groups. However, there have been concerns about the toxicity of full generation dendrimers and risks of premature clearance from circulation, along with other physical drawbacks presented in previous formulations, including large particle sizes and low drug loading efficiency. In our study, carboxyl-terminated PAMAM dendrimer G3.5 was grafted with poly (ethylene glycol) methyl ether (mPEG) to be employed as a nano-based drug delivery system with great cytocompatibility for the delivery of carboplatin (CPT), a widely prescribed anticancer drug with strong side effects so that the drug will be effectively entrapped and not exhibit uncontrolled outflow from the open structure of unmodified PAMAM G3.5. The particles formed were spherical in shape and had the optimal size range (around 36 nm) that accommodates high drug entrapment efficiency. Surface charge was also determined to be almost neutral and the system was cytocompatible. In vitro release patterns over 24 h showed a prolonged CPT release compared to free drug, which correlated to the cytotoxicity assay on malignant cell lines showing the lack of anticancer effect of CPT/mPEG-G3.5 compared with CPT.

scholarly journals Development of Nitazoxanide Loaded Polymeric Nanocarriers: Box Behnken Experimental Design Based Optimisation and Characterisation

2020 ◽  
pp. 34-53
Author(s):  
Charu Bharti ◽  
Shrestha Sharma ◽  
Shobhit Kumar ◽  
Syed Arman Rabbani
Keyword(s):  
Polymeric Nanoparticles ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Poly Vinyl Alcohol ◽  
Cross Linking ◽  
Surface Geometry ◽  
Sustained Drug Release ◽  
Model Drug

The current investigation is focused on formulation, optimisation and characterisation of polymeric based nanomaterial. Nitazoxanide (NTZ) loaded polymeric nanoparticles were prepared by homogenisation technique using Eudragit RL100 as a polymer matrix and Poly vinyl alcohol (PVA) as a cross linking agent. NTZ was used as a model drug and investigated for preformulation parameters along with excipients, identification of concentration for optimization, selection of independent (X) and dependent (Y) variables and characterisation of optimised formulation. Polymeric nanoparticles were obtained after optimization using 33 factorial design by Box Behnken Design expert (BBD). The role and influence of key process variables i.e. concentration of polymer, concentration of cross linking agent and speed of rotation of homogeniser at their respective three different levels for the optimisation of formulation were also investigated. The synthesised optimised polymeric nanoparticles were further characterised by dynamic light scattering (DLS) for its particle size (137.11nm), PDI (0.180) and zeta potential (33.4 mV) while X-ray diffraction (XRD) was used to justify the amorphous and crystalline nature of drug and excipients. Transmission electron microscopy (TEM) further revealed surface geometry of these nanoparticles being spherical in shape, drug entrapment efficiency (%DEE) was found to be 81.89% and in vitro release studies showed sustained drug release effect. The antimicrobial activity against Pseudomonas aeruginosa, Streptococcus mutans and Escherichia coli was also determined.

scholarly journals Design and Evaluation of Microspheres Loaded With Pirenzepine

2018 ◽  
Vol 10 (02) ◽  
Author(s):  
A. Aparna ◽  
C. M. Shalina ◽  
D.V.R.N. Bhikshapathi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Calcium Chloride ◽  
Entrapment Efficiency ◽  
Oral Route ◽  
Cross Linking ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Ich Guidelines

The current objective of the investigation was to fabricate Pirenzepine loaded microspheres for the treatment of gastritis delivered through oral route. The microspheres were prepared by ionotropic gelation technique using sodium as alginate polymer and calcium chloride as cross-linking agent. The effect of polymer and cross-linking agent on particle size, shape, % yield, entrapment efficiency, and drug release were studied. The prepared microspheres morphology and physicochemical properties of were investigated by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Among the total S14 formulations, S7 formulation was optimized at 2.2% of sodium alginate, 7% of calcium chloride maintained100rpm for 10 min at room temperature. The optimized S7 formulation displayed the %EE 94.10%, particle size 82.45 ± 0.09μm, % yield 96.30% and swelling index of 95.13%. From In vitro drug release studies S7 shown 97.17 ± 0.28% up to 12 h in 0.1N HCl, and the drug release followed the zero order and Korsmeyer- Peppas model (R2 = 0.987, 0.995) respectively, indicating the possible drug release mechanism to be by erosion and diffusion. The marketed product showed the drug release of 95.23 ± 0.21% within 1 h. The optimized S7 formulation subjected to stability studies for 6months as per ICH guidelines, no appreciable difference was observed hence the S7 formulation found stable. The data obtained thus suggest that a micro particulate system can be successfully designed for sustained delivery of Pirenzepine and to improve its bioavailability

Application of Methylated N-(4-N,N-Dimethylaminocinnamyl) Chitosan for Oral Protein Drug Delivery

2012 ◽  
Vol 506 ◽  
pp. 465-468
Author(s):  
J. Kowapradit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat ◽  
A. Apirakaramwong ◽  
Warayuth Sajomsang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Entrapment Efficiency ◽  
Egg Yolk ◽  
Molar Ratio ◽  
Protein Drug ◽  
Egg Yolk Phosphatidylcholine ◽  
Model Protein ◽  
Protein Drug Delivery ◽  
Low Cytotoxicity

In the present study, methylated N-(4-N,N-dimethylaminocinnamyl) chitosan (TM65CM50CS) was synthesized and investigated for oral protein drug delivery by combining with liposomes entrapped bovine serum albumin (FITC-BSA), a model protein. FITC-BSA liposomes composed of egg yolk phosphatidylcholine and sodium oleate in molar ratio of 10:2 were prepared by thin film hydration method. The TM65CM50CS coated liposomal FITC-BSA was evaluated for transport of protein and its cytotoxicity in Caco-2 cells. Moreover, the in vitro stability of BSA in TM65CM50CS coated liposomes was also examined by the degradation of protein from pancreatin. The mean particle size and zeta-potential of liposomes were 101+0.02 nm and -27.44+2.02 mV, respectively. Initial FITC-BSA (2.5% w/w) to lipid showed the highest percentage entrapment efficiency (50.13%) and FITC-BSA content (8.08 mg/g of lipid). The results of FITC-BSA transport showed that TM65CM50CS coated FITC-BSA liposomes enhanced protein permeability across Caco-2 cell monolayers with low cytotoxicity. In addition, these liposomes could protect the degradation of protein from pancreatin. Our studies demonstrated that TM65CM50CS coated liposomes have the potential to be used as an oral protein drug delivery.

scholarly journals Preparation of In Situ Cross-Linked N-Maleoyl Chitosan-Oxidized Sodium Alginate Hydrogels for Drug Delivery Applications

2019 ◽  
Vol 7 (21) ◽  
pp. 3546-3553
Author(s):  
Subur P. Pasaribu ◽  
Jamaran Kaban ◽  
Mimpin Ginting ◽  
Jansen Silalahi
Keyword(s):  
Drug Delivery ◽  
Schiff Base ◽  
Sodium Alginate ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Drug Delivery Applications ◽  
Release Profiles

AIM: This study was aimed to prepare in situ cross-linked N-maleoyl chitosan – oxidised sodium alginate (MCS – OSA) hydrogel loaded with metronidazole (MTZ) for drug delivery applications. METHODS: The hydrogel was prepared by in situ cross-linking via Schiff base reaction between amine (-NH2) groups from MCS and aldehyde (-CHO) groups from OSA at the different ratio, and the MTZ was loaded into the hydrogels along with the gelatin processes. RESULTS: The highest drug entrapment efficiency (DEE) was exhibited by MTZ-H3 (5: 5) with DEE of 99.20% and a gel fraction of 97.52%. FTIR results revealed that Schiff base reaction was occurred by the absorption peak of –C = N- groups at 1628 cm-1 and indicated that there is insignificant alteration at different ratio of MCS and OSA. The best sustained of in vitro release profiles of MTZ was shown by MTZ-H3, which is 74.92% and 75.65% at pH 1.2 and 7.4 for 12 h of release, respectively. CONCLUSION: The optimised ratio between MCS and OSA to prepare in situ cross-linked hydrogels were found to be 5:5 according to the results of DEE and in vitro drug release profiles of MTZ and the MTZ loaded MCS-OSA hydrogels have a great potential which can be applied in biomedical applications.

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