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

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.

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Preparation and In-vitro Evaluation of Fe3O4 Encapsulated by Chitosan Loaded Capecitabine Nanoparticles for the Treatment of Breast Cancer

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v6i3.8888 ◽

2016 ◽

Vol 6 (3) ◽

Author(s):

Shanmuganathan S. ◽

Nigma S. ◽

Anbarasan B. ◽

Harika B.

Keyword(s):

Fe3o4 Nanoparticles ◽

Polymer Concentration ◽

In Vitro Release ◽

Entrapment Efficiency ◽

In Vitro Evaluation ◽

Sem Image ◽

Therapeutic Molecules ◽

Dialysis Method ◽

Vitro Release

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.

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Polymeric Nanoparticles of Pistacia lentiscus var. chia Essential Oil for Cutaneous Applications

Pharmaceutics ◽

10.3390/pharmaceutics12040353 ◽

2020 ◽

Vol 12 (4) ◽

pp. 353

Author(s):

Ilianna Vrouvaki ◽

Eleni Koutra ◽

Michael Kornaros ◽

Konstantinos Avgoustakis ◽

Fotini N. Lamari ◽

...

Keyword(s):

Essential Oil ◽

Polymeric Nanoparticles ◽

In Vitro Release ◽

Physicochemical Characteristics ◽

Poly Lactic Acid ◽

Poly Vinyl Alcohol ◽

Pistacia Lentiscus ◽

Shell Material ◽

Sem Images

Polymeric nanoparticles (NPs) encapsulating Pistacia lentiscus L. var. chia essential oil (EO) were prepared by a solvent evaporation method, in order to obtain a novel carrier for administration on the skin. The specific EO exhibits antimicrobial and anti-inflammatory properties thus stimulating considerable interest as a novel agent for the treatment of minor skin inflammations. The incorporation into nanoparticles could overcome the administration limitations that inserts the nature of the EO. Nanoparticles were prepared, utilizing poly(lactic acid) (PLA) as shell material, due to its biocompatibility and biodegradability, while the influence of surfactant type on NPs properties was examined. Two surfactants were selected, namely poly(vinyl alcohol) (PVA) and lecithin (LEC) and NPs’ physicochemical characteristics i.e. size, polydispersity index (PdI) and ζ-potential were determined, not indicating significant differences (p > 0.05) between PLA/PVA-NPs (239.9 nm, 0.081, -29.1 mV) and PLA/LEC-NPs (286.1 nm, 0.167, −34.5 mV). However, encapsulation efficiency (%EE) measured by GC-MS, was clearly higher for PLA/PVA-NPs than PLA/LEC-NPs (37.45% vs. 9.15%, respectively). Moreover PLA/PVA-NPs remained stable over a period of 60 days. The in vitro release study indicated gradual release of the EO from PLA/PVA-NPs and more immediate from PLA/LEC-NPs. The above findings, in addition to the SEM images of the particles propose a potential structure of nanocapsules for PLA/PVA-NPs, where shell material is mainly consisted of PLA, enclosing the EO in the core. However, this does not seem to be the case for PLA/LEC-NPs, as the results indicated low EO content, rapid release and a considerable percentage of humidity detected by SEM. Furthermore, the Minimum Inhibitory Concentration (MIC) of the EO was determined against Escherichia coli and Bacillus subtilis, while NPs, however did not exhibit considerable activity in the concentration range applied. In conclusion, the surfactant selection may modify the release of EO incorporated in NPs for topical application allowing its action without interfering to the physiological skin microbiota.

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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 ◽

10.3390/ma13081989 ◽

2020 ◽

Vol 13 (8) ◽

pp. 1989 ◽

Cited By ~ 1

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.

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Flutamide Loaded Polymeric Nanoparticles for prostate Cancer: A Review

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00782 ◽

2021 ◽

pp. 4501-4503

Author(s):

S. Venkateswara Rao ◽

S. Sathesh Kumar

Keyword(s):

Prostate Cancer ◽

Organic Phase ◽

Polymeric Nanoparticles ◽

Polymer Concentration ◽

Research Work ◽

In Vitro Release ◽

Literature Study ◽

Scientific Publications ◽

Research Perspectives

Flutamide is a potent nonsteroidal anti androgen used to treat advanced prostate cancer. It blocks the androgen receptors on the cancer cells and inhibits the androgen dependent cell growth. This work was planned to compile the research work available in the scientific publications in the formulation and evaluation of Flutamide loaded polymeric nanoparticles for the treating the prostate cancer including the study of influence of various formulation components such as polymer concentration, organic phase volume, drug content, stabilizer concentrations and the ratio between aqueous to organic phase in the characteristics of nanoparticles. Literature study revealed that, methods like Ionic Gelation Technique, Solvent Evaporation method and Nanoprecipitation have been utilized and polymers like Chitosan, casein, Methacrylic acid, PHEA-IB-p(BMA) graft copolymer, mPEG – PLGA and PVA have been utilized. The drug loaded polymeric nanoparticles were evaluated for their physiocochemical properties along with characterization with FTIR, in vitro release and in vitro and in vivo anticancer potential. From the literature it was understood that, nanoprecipitation method was the most commonly used method in various research perspectives. Based on the findings of the present review, Flutamide loaded polymeric nanoparticles may be used as an treatment adjunctive for prostate cancer.

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Development of Rifampicin Nanoparticles by 32 Factorial Design

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2010.3.3.6 ◽

2010 ◽

Vol 3 (3) ◽

pp. 1085-1091

Author(s):

Gambhire Makarand ◽

Vaishali Gambhire ◽

Bhalekar Mangesh

Keyword(s):

Particle Size ◽

Drug Release ◽

Factorial Design ◽

Chemical Interaction ◽

Polymer Concentration ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Plga Nanoparticles ◽

Sustained Drug Release ◽

32 Factorial Design

The preparation and physico-chemical evaluation of rifam-picinloaded poly-(lactic-co-glycolic) acid (PLGA) nanoparticles as per 32 Factorial Design are presented. PLGA (X1) and PVA (Polyvinyl alcohol) solution (X2) as a stabilizing agent were used as independent variables where Particle size (PS) (Y1), Entrapment Efficiency (EE) (Y2) and % Drug Release at 12th h (REL)(Y3) were taken as dependant variables. Rifampicin nanoparticles were prepared by multiple emulsion solvent evaporation method. The results showed the method as reproducible, easy and efficient is the entrapment of drug as well as formation of spherical nanoparticles. Effect of polymer concentration was also evaluated with respect to their % drug entrapment efficiency. The in vitro release studies indicated the rifampicin-loaded PLGA nanoparticles provide sustained drug release over a period of 12h. The optimum batch was R3 which shown particle size 326 nm, 61.70 % EE and 57. 50% drug release at 12th h. Infrared spectroscopy analysis revealed that there was no known chemical interaction between drug and polymer. Hence, this investigation demonstrated the potential of the experimental design in understanding the effect of the formulation variables on the quality of rifampicin nanoparticles.

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Mangiferin-Loaded Polymeric Nanoparticles: Optical Characterization, Effect of Anti-topoisomerase I, and Cytotoxicity

Cancers ◽

10.3390/cancers11121965 ◽

2019 ◽

Vol 11 (12) ◽

pp. 1965 ◽

Cited By ~ 2

Author(s):

Francisco Fabian Razura-Carmona ◽

Alejandro Pérez-Larios ◽

Napoleón González-Silva ◽

Mayra Herrera-Martínez ◽

Luis Medina-Torres ◽

...

Keyword(s):

Topoisomerase I ◽

Polymeric Nanoparticles ◽

Biological Activities ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Plga Nanoparticles ◽

Encapsulation Process ◽

Mean Size ◽

High Concentrations

Mangiferin is an important xanthone compound presenting various biological activities. The objective of this study was to develop, characterize physicochemical properties, and evaluate the anti-topoisomerase activity of poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing mangiferin. The nanoparticles were developed by the emulsion solvent evaporation method and the optimal formulation was obtained with a response surface methodology (RSM); this formulation showed a mean size of 176.7 ± 1.021 nm with a 0.153 polydispersibility index (PDI) value, and mangiferin encapsulation efficiency was about 55%. The optimal conditions (6000 rpm, 10 min, and 300 μg of mangiferin) obtained 77% and the highest entrapment efficiency (97%). The in vitro release profile demonstrated a gradual release of mangiferin from 15 to 180 min in acidic conditions (pH 1.5). The fingerprint showed a modification in the maximum absorption wavelength of both the polymer and the mangiferin. Results of anti-toposiomerase assay showed that the optimal formulation (MG4, 25 µg/mL) had antiproliferative activity. High concentrations (2500 µg/mL) of MG4 showed non-in vitro cytotoxic effect on BEAS 2B and HEPG2. Finally, this study showed an encapsulation process with in vitro gastric digestion resistance (1.5 h) and without interfering with the metabolism of healthy cells and their biological activity.

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Evaluation of the Hemocompatibility and Anticancer Potential of Poly(ε-Caprolactone) and Poly(3-Hydroxybutyrate) Microcarriers with Encapsulated Chrysin

Pharmaceutics ◽

10.3390/pharmaceutics13010109 ◽

2021 ◽

Vol 13 (1) ◽

pp. 109

Author(s):

Eleftherios Halevas ◽

Chrysoula Kokotidou ◽

Elda Zaimai ◽

Alexandra Moschona ◽

Efstratios Lialiaris ◽

...

Keyword(s):

Blood Compatibility ◽

Hematological Parameters ◽

In Vitro Release ◽

Cancer Cell Line ◽

Entrapment Efficiency ◽

Morphological Properties ◽

Poly Vinyl Alcohol ◽

Loading Capacity ◽

The Novel

In this work, novel chrysin-loaded poly(ε-caprolactone) and poly(3-hydroxybutyrate) microcarriers were synthesized according to a modified oil-in-water single emulsion/solvent evaporation method, utilizing poly(vinyl alcohol) surfactant as stabilizer and dispersing agent for the emulsification, and were evaluated for their physico-chemical and morphological properties, loading capacity and entrapment efficiency and in vitro release of their load. The findings suggest that the novel micro-formulations possess a spherical and relatively wrinkled structure with sizes ranging between 2.4 and 24.7 µm and a highly negative surface charge with z-potential values between (−18.1)–(−14.1) mV. The entrapment efficiency of chrysin in the poly(ε-caprolactone) and poly(3-hydroxybutyrate) microcarriers was estimated to be 58.10% and 43.63%, whereas the loading capacity was found to be 3.79% and 15.85%, respectively. The average release percentage of chrysin was estimated to be 23.10% and 18.01%, respectively. The novel micromaterials were further biologically evaluated for their hemolytic activity through hemocompatibility studies over a range of hematological parameters and cytoxicity against the epithelial human breast cancer cell line MDA-MB 231. The poly(ε-caprolactone) and poly(3-hydroxybutyrate) microcarriers reached an IC50 value with an encapsulated chrysin content of 149.19 µM and 312.18 µM, respectively, and showed sufficient blood compatibility displaying significantly low (up to 2%) hemolytic percentages at concentrations between 5 and 500 µg·mL−1.

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STUDIES ON NANOLIPID EMULGEL OF NIMESULIDE FOR TRANSDERMAL DELIVERY

INDIAN DRUGS ◽

10.53879/id.56.09.11336 ◽

2019 ◽

Vol 56 (09) ◽

pp. 74-77

Author(s):

C Trimukhe ◽

P. Patil ◽

K. Sheth ◽

N. Desai ◽

Keyword(s):

Ex Vivo ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Spherical Particles ◽

Sustained Drug Release ◽

Polyethylene Glycol 400 ◽

Ex Vivo Permeation ◽

Nanometric Range ◽

Permeation Studies

The objective of the present study was to develop and evaluate a nanolipid transdermal emulgel of Nimesulide. The nanolipid particles of Nimesulide were developed using Compritol 888 ATO and Labrafil M1944 as lipids, Polysorbate 80 as surfactant with Poloxamer 188 and Polyethylene Glycol 400 as stabilizer and cosolvent respectively. The nanoparticles were developed by Hot Nanoemulsification Low Temperature Solidification method and showed drug entrapment efficiency of 67 ± 2.316 % with particle size of 500 – 600 nm. TEM studies indicated presence of spherical particles in the nanometric range. The nanolipidic dispersions were suitably gelled to form emulgel. The in vitro release of the developed emulgel showed sustained drug release for 8 hours with no evidence of toxicity during histopathological testing after ex vivo permeation studies. The nanolipid emulgel of Nimesulide can thus provide sustained release action due to enhanced skin deposition for effective treatment of chronic arthritic conditions, thereby improving patient compliance.

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FORMULATION, CHARACTERIZATION AND IN VITRO EVALUATION OF FLOATING MICROSPHERES OF MEBENDAZOLE AS A GASTRO RETENTIVE DOSAGE FORM

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5-s.1980 ◽

2018 ◽

Vol 8 (5-s) ◽

pp. 311-314

Author(s):

Lokesh Parmar ◽

Mansi Gupta ◽

Geeta Parkhe

Keyword(s):

Ethyl Cellulose ◽

Release Kinetics ◽

In Vitro Release ◽

Methyl Cellulose ◽

Entrapment Efficiency ◽

Drug Bioavailability ◽

Evaporation Method ◽

Solvent Diffusion ◽

Model Drug

The present study involves preparation and evaluation of floating microspheres using Mebendazole (MBZ) as a model drug for improving the drug bioavailability by prolongation of gastric retention time. Ethyl cellulose, hydroxyl propyl methyl cellulose microspheres loaded with mebendazole were prepared by solvent diffusion evaporation method. The microspheres had smooth surfaces, with free-flowing and good-packing properties. The yield of the microspheres was up to 85.65±0.14% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in the range 215.1 to 251.80 nm. The prepared microspheres exhibited prolonged drug release and Percentage buoyancy was found to70.25±0.15. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to Stability studies and In-vitro release and Release kinetics data was subjected to different dissolution models. Keywords: solvent diffusion evaporation method, Mebendazole, Ethyl cellulose, Hydroxyl propyl methyl cellulose

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DEVELOPMENT OF GASTRO-RETENTIVE FLOATING MICROSPHERES OF ONDANSETRON HYDROCHLORIDE

INDIAN DRUGS ◽

10.53879/id.51.08.10142 ◽

2014 ◽

Vol 51 (08) ◽

pp. 22-27

Author(s):

S. G Bandbe ◽

◽

K Dixit ◽

G Laghate ◽

R. B. Athawale

Keyword(s):

Particle Size ◽

Drug Release ◽

Ethyl Cellulose ◽

Polymer Concentration ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Ondansetron Hydrochloride ◽

Percentage Yield ◽

Gastro Retentive

Ondansetron hydrochloride (OND) is indicated for prevention of nausea and vomiting during chemotherapy. Due to its insolubility in intestinal pH, it is absorbed only in the stomach. In the present study, an attempt was made to increase gastric retention time of ondansetron hydrochloride by preparing its floating microspheres by solvent evaporation method with ethyl cellulose (EC) and hydroxypropylmethylcellulose (HPMC). Microspheres were characterized for percentage yield, particle size, surface morphology, floating behaviour, entrapment efficiency and in vitro release. Polymer ratio and stirring speed seemed to have significant impact on size, entrapment efficiency, floating time and release profile. Hydroxypropylmethylcellulose: ethyl cellulose in the ratio 1: 3, gave most suitable buoyancy and drug release. By increasing polymer concentration, the mean particle size of microspheres increased while drug release rate decreased. Developed formulation of ondansetron hydrochloride can be used for prolonging its retention in the stomach for at least 12 hrs, thereby improving bioavailability and patient compliance.

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