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.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Anti-Inflammatory and Gastroprotective Properties of Aspirin - Entrapped Solid Lipid Microparticles

2020 ◽  
Vol 14 (1) ◽  
pp. 78-88
Author(s):  
Salome A. Chime ◽  
Paul A. Akpa ◽  
Cosmas C. Ugwuanyi ◽  
Anthony A. Attama
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Particle Size Range ◽  
Simulated Intestinal Fluid ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles ◽  
Anti Inflammatory ◽  
Gastric Irritation

Background: Aspirin is a nonsteroidal anti-inflammatory drug that is very effective in the treatment of inflammation and other health conditions, however, it causes gastric irritation. Recently, researchers have developed patents (US9757529, 2019) of inhalable aspirin for rapid absorption and circumvention of gastric irritation. Objective: The aim of this work was to formulate aspirin-loaded lipid based formulation in order to enhance oral bioavailability and inhibit gastric irritation. Methods: This solid lipid microparticles loaded with aspirin (SLM) was formulated by a modified cold homogenization-solvent evaporation method. In vitro studies such as in vitro drug release, particle size, Encapsulation Efficiency (EE), micromeritic properties and loading capacity were carried out. Pharmacodynamics studies such as anti-inflammatory and ulcerative properties of the SLM were also carried out in Wistar rats. Results: The results showed that aspirin entrapped SLM exhibited the highest EE of 72% and particle size range of 7.60 + 0.141µm to 20.25 + 0.070µm. Formulations had about 55% drug release at 6h in simulated intestinal fluid pH 6.8. The formulations had good flowability that could facilitate filling into hard gelatin capsule shells. The SLM exhibited 100% gastroprotection against aspirin-induced ulcers (p < 0.05). The percentage of anti-inflammatory activities also showed that aspirin-entrapped SLM had 78% oedema inhibition at 7h, while the reference had 68% inhibition at 7h. Conclusion: Aspirin-entrapped SLM showed good sustained-release properties, enhanced antiinflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.

Folate conjugated solid lipid nanoparticle: formulation development, optimization and characterization

2021 ◽  
Vol 11 ◽  
Author(s):  
Vaibhav Rajoriya ◽  
Varsha Kashaw ◽  
Sushil Kumar Kashaw
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Release Study

Objective: The current paper represents the development, optimization, and characterization of paclitaxel-loaded folate conjugated solid lipid nanoparticles (FA-SLNs). Methods: The ligand (FA-SLNs) conjugated and non-conjugated SLNs (PTX-SLNs) were prepared by hot homogenization method. Both of the formulations (FA-SLNs and PTX-SLNs) were optimized with various parameters i.e. drug loading, stirring time, stirring speed, particle size, and polydispersity index, and characterized. The in-vitro drug release study was performed in different pH environments by using the dialysis bag method. The surface morphology and particle size were determined through scanning electron micorscopy and Transmission Electron Microscopy respectively, The SLNs formulations were also evaluated for the stability study. Result: The particle size of PTX-SLNs and FA-SLNs was determined and found to be 190.1±1.9 and 231.3±2.3 nm respectively. The surface morphology of the SLNs indicates that the prepared formulations are round-shaped and show smooth surfaces. The TEM study indicated that particles were in the range of 100-300 nm. The entrapment efficiency and drug loading capacity of FA-SLNs were found to be 79.42±1.6% and 17.3±1.9%, respectively. In-vitro drug release study data, stated that the optimum drug release was found in an acidic environment at pH 4.0, that showed 94.21% drug release after 16 hours and it proves that optimized formulation FA-SLNs will gave the sustained and better release in tumor tissue that owing acidic environment because of the angiogenesis process. Conclusion: In this research paper, different formulation parameters, found to influence fabrication of drug into Solid lipid nanoparticles, were optimized for high entrapment efficiency and drug loading. The most important parameters were drug:lipid ratio, drug:polymer ratio and lipid: surfactant ratio. Higher in-vitro drug release was observed in pH 4 as compared to the pH 7.4. These result data concludes that FA-SLNs formulation was successfully prepared, optimized and characterized.

Formulation Development and Characterization of Solid Lipid Nanoparticles Containing Nimesulide

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Jain Pushpendra ◽  
Mishra Amit ◽  
Yadav K. ◽  
Patil K. ◽  
Baghel S.
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Average Diameter ◽  
Controlled Drug Release ◽  
Lipid Nanoparticles ◽  
Formulation Development ◽  
Solid Lipid

The aim of this study was to prepare nimesulide solid lipid nanoparticles (NIM-SLNs), to formulate the controlled drug release and to evaluate its physiochemical characteristics. NIM-SLNs were prepared by an emulsification and low-temperature solidification method. Additionally, attempts have been made to study the effect of individual process parameters (stirring speed and stirring time) and formulation parameters (Lecithin concentration, drug concentration and surfactant concentration) on entrapment efficiency. An approximately entrapment efficiency of (60%) and an average drug loading of (1.0 %) were achieved from optimized formulation of NIM-SLNs. The results show that the TMZ-SLNs had an average diameter of 187±1.23nm and in vitro drug release was conducted in phosphate-buffered saline (pH 7.4) at 37oC. The cumulative percentages drug release of nimesulide was found approximately 60% in 24 hours and release behavior was in accordance with Higuchi-equation. The results indicate that the SLNs is a promising controlled-release system. It may also allow a reduction in dosage and a decrease in systemic toxicity.

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.

scholarly journals FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

2021 ◽  
pp. 216-226
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Sustained Drug Delivery ◽  
Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

scholarly journals FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Polyvinyl Pyrrolidone ◽  
Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

scholarly journals Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 870 ◽  
Author(s):  
Clara López-Iglesias ◽  
Cristina Quílez ◽  
Joana Barros ◽  
Diego Velasco ◽  
Carmen Alvarez-Lorenzo ◽  
...  
Keyword(s):  
Skin Barrier ◽  
Wound Dressings ◽  
Wound Complications ◽  
In Vitro Test ◽  
Skin Substitutes ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Lipid Microparticles ◽  
Saturated Solutions

The delivery of bioactive agents using active wound dressings for the management of pain and infections offers improved performances in the treatment of wound complications. In this work, solid lipid microparticles (SLMPs) loaded with lidocaine hydrochloride (LID) were processed and the formulation was evaluated regarding its ability to deliver the drug at the wound site and through the skin barrier. The SLMPs of glyceryl monostearate (GMS) were prepared with different LID contents (0, 1, 2, 4, and 10 wt.%) using the solvent-free and one-step PGSS (Particles from Gas-Saturated Solutions) technique. PGSS exploits the use of supercritical CO2 (scCO2) as a plasticizer for lipids and as pressurizing agent for the atomization of particles. The SLMPs were characterized in terms of shape, size, and morphology (SEM), physicochemical properties (ATR-IR, XRD), and drug content and release behavior. An in vitro test for the evaluation of the influence of the wound environment on the LID release rate from SLMPs was studied using different bioengineered human skin substitutes obtained by 3D-bioprinting. Finally, the antimicrobial activity of the SLMPs was evaluated against three relevant bacteria in wound infections (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa). SLMPs processed with 10 wt.% of LID showed a remarkable performance to provide effective doses for pain relief and preventive infection effects.

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