scholarly journals Sustained release biodegradable solid lipid microparticles: Formulation, evaluation and statistical optimization by response surface methodology

2017 ◽  
Vol 67 (4) ◽  
pp. 441-461
Author(s):  
Muhammad Hanif ◽  
Hafeez Ullah Khan ◽  
Samina Afzal ◽  
Asif Mahmood ◽  
Safirah Maheen ◽  
...  
Keyword(s):  
Entrapment Efficiency ◽  
Quadratic Model ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Glyceryl Monostearate ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles ◽  
The Impact ◽  
Central Composite

Abstract For preparing nebivolol loaded solid lipid microparticles (SLMs) by the solvent evaporation microencapsulation process from carnauba wax and glyceryl monostearate, central composite design was used to study the impact of independent variables on yield (Y1), entrapment efficiency (Y2) and drug release (Y3). SLMs having a 10-40 μm size range, with good rheological behavior and spherical smooth surfaces, were produced. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry pointed to compatibility between formulation components and the zeta-potential study confirmed better stability due to the presence of negative charge (-20 to -40 mV). The obtained outcomes for Y1 (29-86 %), Y2 (45-83 %) and Y3 (49-86 %) were analyzed by polynomial equations and the suggested quadratic model were validated. Nebivolol release from SLMs at pH 1.2 and 6.8 was significantly (p < 0.05) affected by lipid concentration. The release mechanism followed Higuchi and zero order models, while n > 0.85 value (Korsmeyer- Peppas) suggested slow erosion along with diffusion. The optimized SLMs have the potential to improve nebivolol oral bioavailability.

scholarly journals Formulation Design and Evaluation of Solid Lipid Micro-particles of Curcumin for the Treatment of Alzheimer’s disease

2020 ◽  
Vol 11 (4) ◽  
pp. 6739-6747
Author(s):  
Amin Mir M ◽  
Muhammad Waqar Ashraf ◽  
Maythem Mahmud
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Compatibility Study ◽  
Cumulative Release ◽  
Solid Lipid ◽  
Micro Particles ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles

Solid lipid microparticles reach the site of its action in a controlled rate and do show controlled release for a better therapeutic result. A good drug carrying and release system involve a controlled drug delivery that improves bioavailability, to enrich stability and to minimise the toxic effects followed with a targeted drug at the site of its action. The solid lipid microparticles of curcumin were prepared in a view to achieving high permeability of curcumin in the brain through blood-brain-barrier. The lipid microsphere solids were prepared by hot melts microencapsulation technique to formulate solid lipid microspheres. Twelve lipid formulations were prepared with varying concentration of surfactants (span 40, span 70, span 90 and Tween 100). The developed formulation was subjected to various parameters such as the particle size, % entrapment efficiencies, yield productions, % cumulative release, percentage yield and drug loading, based upon highest entrapment efficiency, drug release and % cumulative release, the F3 formulation was considered as the best formulation. The prepared microsphere was subjected to different evaluation parameters such as thin-layer chromatography, melting point, FTIR, solubility, compatibility study and In-vitro drug release. The developed formulation shows spherical and smooth surface. The percentage release of drug F3 formulation has been found highest of about 86.23% after 12 hr.

Design and Optimization of Itraconazole Loaded SLN for Intranasal Administration Using Central Composite Design

2020 ◽  
Vol 10 (6) ◽  
pp. 884-891
Author(s):  
Sarvjeet S. Rana ◽  
Shailendra Bhatt ◽  
Manish Kumar ◽  
Anuj Malik ◽  
Jai B. Sharma ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Intranasal Administration ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Ex Vivo Study ◽  
Central Composite

Introduction: Solid Lipid nanoparticles (SLN) are comprising of a solid lipid core with a mean diameter between 50 and 1000 nm. SLN is an advanced carrier system to traditional colloidal carriers such as emulsion, liposomes, and polymeric microparticles. Objective: The objective of this study was to formulate SLN of Itraconazole (ITZ) for intranasal administration. Methods: ITZ-loaded SLN were prepared by high pressure homogenization technique using the Central Composite Design (CCD). The concentration of surfactant (X1) and drug to lipid ratio (X2) was considered as independent variables, whereas particle size (Y1) and percentage entrapment efficiency (Y2) were considered as a response. The compatibility of ingredients with the drug was tested using differential scanning calorimetry. SLN were characterized for their particle size, entrapment efficiency, transmission electron microscopy, in vitro drug release, and ex vivo study. Results: The solid lipid nanoparticles were successfully prepared using high pressure homogenization technique and glyceryl monostearate was used as solid lipid. The lipid ratio significantly increases the particle size as well as entrapment efficiency. The particle size and (%) entrapment efficiency of optimized formulation were found to be 29 nm and 78.9%, respectively. The differential scanning calorimetry confirmed that the drug existed in amorphous form. Nasal histopathology study on sheep mucosa revealed that the developed SLN was non-toxic and safe to use for intranasal administration. The results of ex vivo study showed that the Higuchi pattern of drug release was followed. The in vitro release studies showed the significant difference in drug release from ITZ-loaded SLN compared to plain ITZ-solution. Conclusion: ITZ-loaded SLN were successfully prepared and validated. The best batch was selected based on the desired particle size, and EE which is an important characteristic for SLN formulations. The developed formulations were nontoxic as determined by histo-pathological studies.

scholarly journals Physicochemical Characterization of Artemether-Entrapped Solid Lipid Microparticles Prepared from Templated- Compritol and Capra hircus (Goat Fat) Homolipid

2021 ◽  
Vol 20 (1) ◽  
pp. 67-80
Author(s):  
Petra Obioma Nnamani ◽  
Franklin Chimaobi Kenechukwu ◽  
Chinekwu Sheridan Nwagwu ◽  
Onyinye Okoye ◽  
Anthony Amaechi Attama
Keyword(s):  
Physicochemical Properties ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Capra Hircus ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Simulated Intestinal Fluid ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles

The purpose of this study was to formulate and evaluate the physicochemical properties of artemetherloaded solid lipid microparticles (SLM) prepared from templated-compritol 888®ATO and Capra hircus (goat fat) homolipid. Various ratios of compritol 888®ATO, goat fat and Phospholipon® 90G were used to prepare the templated lipid matrices and characterized by differential scanning calorimetry (DSC). Plain and artemether-loaded SLM (0, 1.0, 3.0 and 5.0% drug) were prepared by melt-homogenization. The SLM were characterized regarding the compatibility by DSC, morphology and particle size by polarized light microscopy (PLM), encapsulation efficiency (EE%), in vitro release in simulated gastric fluid (SGF, pH 1.2), simulated intestinal fluid (SIF, pH 7.2) and alcoholic buffer (pH 3.6), and time-resolved pH-dependent stability. Stable, smooth and mostly spherical SLM with particle sizes in the range 18.77-43.79 μm and EE% ranging from 62.22% to 99.05% were obtained. DSC results showed the compatibility of drug and the formulation excipients as well as the stability of artemether in the developed SLM. Results showed significantly (p<0.05) higher drug release (88.25%) in alcoholic buffer than in SIF and SGF. By implication, incorporation of alcohol in the formulation would be a practical approach to improve artemether bioavailability from the SLM. This study has shown that the physicochemical properties of artemether were improved by SLM based on templated-compritol 888®ATO and goat fat. Dhaka Univ. J. Pharm. Sci. 20(1): 67-80, 2021 (June)

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Development and characterization of solid lipid microparticles loaded with ascorbic acid and produced by spray congealing

2015 ◽  
Vol 67 ◽  
pp. 52-59 ◽  
Author(s):  
Fernando Eustáquio Matos-Jr ◽  
Marcello Di Sabatino ◽  
Nadia Passerini ◽  
Carmen Sílvia Favaro-Trindade ◽  
Beatrice Albertini
Keyword(s):  
Ascorbic Acid ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles

Mannosylated Solid Lipid Nanocarriers Of Chrysin To Target Gastric Cancer: Optimization and Cell line Study.

2021 ◽  
Vol 18 ◽  
Author(s):  
Sonia S. Pandey ◽  
Farhinbanu I. Shaikh ◽  
Arti R. Gupta ◽  
Rutvi J. Vaidya
Keyword(s):  
Gastric Cancer ◽  
Particle Size ◽  
Ex Vivo ◽  
Biological Effects ◽  
Entrapment Efficiency ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Lipid Nanocarriers

Background: Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability. Objective: The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer. Methods: The Chrysin loaded SLNs (C-SLNs) were developed optimized, characterized and further mannosylated. The C-SLNs were developed with high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines. Results: DSC and XRD data predict the chrysin encapsulation in lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in dependent variable - increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs. Conclusion: These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat the gastric cancer.

scholarly journals Preparation, characterization and scale-up of sesamol loaded solid lipid nanoparticles

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Scale Up ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Transmission Electron ◽  
The Brain

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.

Solid lipid microparticles loaded with cinnamon oleoresin: Characterization, stability and antimicrobial activity

2018 ◽  
Vol 113 ◽  
pp. 351-361 ◽  
Author(s):  
Fernanda Ramalho Procopio ◽  
Vivian Boesso Oriani ◽  
Bruno Nicolau Paulino ◽  
Leonardo do Prado-Silva ◽  
Glaucia Maria Pastore ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles

scholarly journals Formulation And Evaluation Of Acyclovir Sodium Solid Lipid Microparticles

2016 ◽  
Vol 04 (05) ◽  
Author(s):  
Anantha Naik Nagappa ◽  
Gaurav Agarwal ◽  
Vinuth Chikkamath ◽  
Shilpi Agarwal ◽  
Rekha Rani ◽  
...  
Keyword(s):  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles

scholarly journals Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

2013 ◽  
Vol 63 (4) ◽  
pp. 517-529 ◽  
Author(s):  
Emrah Korkm ◽  
Evren H. Gokce ◽  
Ozgen Ozer
Keyword(s):  
Coenzyme Q10 ◽  
High Speed ◽  
Antioxidant Properties ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Scanning Calorimetry ◽  
Transmission Electron Microscopy Analysis ◽  
Solid Lipid

Abstract Coenzyme Q10 (Q10) loaded solid lipid nanoparticles (SLN) were prepared by the high speed homogenization method and incorporated into Carbopol 974P hydrogels. Compritol 888 ATO (C888) was employed as the lipid base; Poloxamer 188 (P188) and Tween 80 (Tw80) were used as surfactant and co-surfactant. Optimum particle size with narrow distribution was obtained as 152.2 nm for blank and 142.4 nm for Q10 loaded SLNs. The overall charge of loaded SLNs was -13.7 ± 1.3 mV. Q10 entrapment efficiency was 89 % and the production yield was 94 %. Transmission electron microscopy analysis provided evidence of colloidal size, spherical shape while differential scanning calorimetry analysis confirmed recrystallization of the lipid after the preparation of SLNs. Trolox equivalent antioxidant capacity (TEAC) analysis has shown that antioxidant potential of Q10 can be protected in SLNs. Rheological characteristics demonstrated that the SLN incorporating gels were shear thinning and the mechanical strength of the gels was suitable for topical application. Diffusion studies from rat abdominal skin revealed that the delivery of Q10 was doubled in SLN incorporating gels, approximately 40 μg cm-2, in comparison with gels prepared with only Q10 (not incorporated in SLNs). As a result, it can be stated that Q10-SLN loaded gels can be successful delivery systems for carrying Q10 efficiently into the skin without losing its antioxidant properties.

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