Preparation and Characterization of Solid Lipid Nanoparticles of Cinnacalcet HCl

Objective: The objective of the present research is to formulate solid lipid nanoparticles of cinnacalcet HCl to improve its oral bioavailability. Methods: Cinnacalcet hydrochloride exhibits poor oral bioavailability of 20 to 25 % because of low aqueous solubility and first pass metabolism. The formulations were optimised using Box-Behnken Design. Solid lipid nanoparticles formulation was prepared using hot homogenization and ultra sonication method. Results and Discussion: Precirol ATO 05, Soya lecithin and poloxamer 407 were selected as lipid, surfactant and co-surfactant respectively. For optimistaion the desirable goal was fixed for various responses entrapment efficiency, particle size and (time taken for diffusion of 85% drug) T85%. The optimized single dose of solid lipid nanoparticle obtained using box behnken design consisting of 30 mg of cinnacalcet HCl, 200 mg of precirol ATO 05, 250 mg of soya lecithin and 0.2% w/v of poloxamer. 407. The pharmacokinetic study revealed that optimized formulation was found to increase the oral bioavailability nearly 3 times compared to aqueous suspension of pure drug. Conclusion: Thus optimized solid lipid nanoparticle explicated the potential of lipid-based nanoparticles as a potential carrier in improving the oral delivery.

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Development of Dithranol overloaded hard Lipid Nanoparticles

International Journal of Pharmacy and Biomedical Engineering ◽

10.14445/23942576/ijpbe-v2i3p102 ◽

2015 ◽

Vol 2 (3) ◽

pp. 5-8

Author(s):

Anahera C ◽

Kahurangi S

Keyword(s):

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Solid Lipid Nanoparticle ◽

Ftir Study ◽

Psoriasis Treatment ◽

Solubility Study ◽

Solid Lipid ◽

Lipid Nanoparticle ◽

Preformulation Studies ◽

Hplc Study

Dithranol belongs to the keratolytic category, which is widely used drug in the treatment of psoriasis. The drug is virtually inexplicable in water. Many conservative quantity forms for psoriasis treatment have been have been formulated earlier, but they did not show good results. Hence in the present study, it was attempted to invent dithranol in the form of solid lipid nanoparticle. Solid lipid nanoparticles of dithranol were obtained by alteration of lipid spreading method. Preformulation studies were performed to check the compatibility of drug and excepient for the development of formulation by DSC and no statement was found. Solubility study, division coefficient purpose, UV examination, HPLC study, FTIR study were also performed. After the preformulation studies Dithranol loaded solid lipid nanoparticles was also prepared. Hence it was concluded that solid lipid nanoparticle of dithranol could be formulated.

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Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i3.2849 ◽

2019 ◽

Vol 9 (3) ◽

pp. 212-221 ◽

Cited By ~ 2

Author(s):

Aparna Bhalerao ◽

Pankaj Prakash Chaudhari

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

Encapsulation Efficiency ◽

Drug Loading ◽

Lipid Nanoparticles ◽

Water Soluble ◽

Solid Lipid Nanoparticle ◽

Solid Lipid ◽

Lipid Nanoparticle

Cilinidipine is a fourth generation N and L-type calcium channel antagonists used alone or in combination with another drug to treat hypertension. Cilnidipine is poorly water -soluble, BCS class II drug with 6 to 30 percent oral bioavailability due to first pass metabolism. So to protect the drug from degradation and improve its dissolution, solid lipid nanoparticles were prepared. Glyceryl monostearate was selected as lipid while span 20: tween 20 were selected as surfactant blends. The formulations were evaluated for various parameters, as percent transmittance, drug content, percent encapsulation efficiency; percent drug loading, In vitro drug release and particle size. Optimized formulation was lyophilized using lactose as a cryo-protectant. The lyophilized formulation was evaluated for micromeritic properties, particle size and in vitro dissolution. It was further evaluated for DSC, XRD, and SEM. Percent encapsulation efficiency and percent drug loading of optimized formulation (F3) were 78.66percent and 9.44percent respectively. The particle size of F3 formulation without drug was 204 nm and with the drug was 214 nm. The particle size of the reconstituted SLN was 219 nm. In DSC study, no obvious peaks for cilnidipine were found in the SLN of cilnidipine indicated that the cilnidipine must be present in a molecularly dissolved state in SLN. In X-ray diffractometry absence of peaks representing crystals of cilnidipine in SLN indicated that the drug was in an amorphous or disordered crystalline phase in the lipid matrix. Thus, solid lipid nanoparticle formulation is a promising way to enhance the dissolution rate of cilnidipine. Keywords: Cilnidipine, Solid Lipid Nanoparticle, Hypertension

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Development of a topical adapalene-solid lipid nanoparticle loaded gel with enhanced efficacy and improved skin tolerability

RSC Advances ◽

10.1039/c5ra06047h ◽

2015 ◽

Vol 5 (55) ◽

pp. 43917-43929 ◽

Cited By ~ 19

Author(s):

Harshad Harde ◽

Ashish Kumar Agrawal ◽

Mahesh Katariya ◽

Dnyaneshwar Kale ◽

Sanyog Jain

Keyword(s):

Solid Lipid Nanoparticles ◽

Skin Irritation ◽

Lipid Nanoparticles ◽

Solid Lipid Nanoparticle ◽

Solid Lipid ◽

Lipid Nanoparticle ◽

Skin Tolerability

The present investigation substantiates the efficacy of adapalene loaded solid lipid nanoparticles (Ada-SLNs) in ameliorating the skin irritation potential of adapalene owing to its altered skin distribution.

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Formulation and evaluation of prazosin hydrochloride loaded solid lipid nanoparticles

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i6-s.2170 ◽

2018 ◽

Vol 8 (6-s) ◽

pp. 63-69

Author(s):

Sandip Akaram Bandgar ◽

Pranali Dhavale ◽

Pravin Patil ◽

Sardar Shelake ◽

Shitalkumar Patil

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

Entrapment Efficiency ◽

Aqueous Solubility ◽

Lipid Nanoparticles ◽

Solid Lipid Nanoparticle ◽

Bioavailability Enhancement ◽

Solid Lipid ◽

Lipid Nanoparticle ◽

Optimum Stability

Solid Lipid Nanoparticles (SLN) are rapidly developing field of nanotechnology with several potential application in drug delivery and research. Drugs having low aqueous solubility not only give low oral bioavailability but provide high inter-and intra subject variability. The purpose of the present study was to investigate the bioavailability enhancement of Prazosin Hydrochloride drug by formulating solid lipid nanoparticle. Prazosin Hydrochloride Drug is an antihypertensive drug with limited bioavailability so that solid lipid nanoparticle (SLN) is one of the approaches to improve bioavailability. SLN were prepared using glyceryl monostearate by hot homogenization followed by Solvent emulsification-ultrasonication. Prazosin Hydrochloride loaded SLN were characterized and optimized by parameters like particle size, zeta potential, XRD, DSC. Proposing Hydrochloride loaded SLN having the particle size 263.8±1.88 and entrapment efficiency 89.29±0.65% shows better bioavailability and optimum stability in studies. The SLN studies prepared using glyceryl mono stearate as a lipid and Polaxamer 407 as a polymer leads to improve bioavailability of the drug. Keywords: Prazosin Hydrochloride, Solid Lipid Nanoparticles, Entrapment efficiency, DSC

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Short Term Stability Testing of Efavirenz-Loaded Solid Lipid Nanoparticle (SLN) and Nanostructured Lipid Carrier (NLC) Dispersions

Pharmaceutics ◽

10.3390/pharmaceutics11080397 ◽

2019 ◽

Vol 11 (8) ◽

pp. 397 ◽

Cited By ~ 11

Author(s):

Pedzisai A. Makoni ◽

Kasongo Wa Kasongo ◽

Roderick B. Walker

Keyword(s):

Solid Lipid Nanoparticles ◽

Encapsulation Efficiency ◽

Lipid Nanoparticles ◽

Nanostructured Lipid Carriers ◽

Nanostructured Lipid Carrier ◽

Solid Lipid Nanoparticle ◽

Short Term ◽

Term Stability ◽

Solid Lipid ◽

Lipid Nanoparticle

The short term stability of efavirenz-loaded solid lipid nanoparticle and nanostructured lipid carrier dispersions was investigated. Hot High Pressure Homogenization with the capability for scale up production was successfully used to manufacture the nanocarriers without the use of toxic organic solvents for the first time. Glyceryl monostearate and Transcutol® HP were used as the solid and liquid lipids. Tween® 80 was used to stabilize the lipid nanocarriers. A Box-Behnken Design was used to identify the optimum operating and production conditions viz., 1100 bar for 3 cycles for the solid lipid nanoparticles and 1500 bar for 5 cycles for nanostructured lipid carriers. The optimized nanocarriers were predicted to exhibit 10% efavirenz loading with 3% and 4% Tween® 80 for solid lipid nanoparticles and nanostructured lipid carriers, respectively. Characterization of the optimized solid lipid nanoparticle and nanostructured lipid carrier formulations in relation to shape, surface morphology, polymorphism, crystallinity and compatibility revealed stable formulations with particle sizes in the nanometer range had been produced. The nanocarriers had excellent efavirenz loading with the encapsulation efficiency >90%. The optimized nanocarriers exhibited biphasic in vitro release patterns with an initial burst release during the initial 0–3 h followed by sustained release over a 24 h period The colloidal systems showed excellent stability in terms of Zeta potential, particle size, polydispersity index and encapsulation efficiency when stored for 8 weeks at 25 °C/60% RH in comparison to when stored at 40 °C/75% RH. The formulations manufactured using the optimized conditions and composition proved to be physically stable as aqueous dispersions.

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Surface Modification of Optimized Asenapine Maleate Loaded Solid Lipid Nanoparticles Using Box-Behnken Design

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i31b31706 ◽

2021 ◽

pp. 176-193

Author(s):

A. Rekha Devi ◽

M. Vidyavathi ◽

S. P. Suryateja

Keyword(s):

Surface Modification ◽

Drug Release ◽

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Brain Targeting ◽

Average Particle ◽

Box Behnken Design ◽

Solid Lipid

Aim: The aim of the present study was to design and evaluate solid lipid nanoparticles of Asenapine maleate (<2% bioavailability) to enhance its oral bioavailability and surface modification for brain targeting. Methods: A modified solvent injection method was used to produce Asenapine maleate loaded solid lipid nanoparticles. A RSM 3-factor, 3-level Box-Behnken design was applied to study the effect of three independent variables, concentrations of lipid (A), drug (B) and surfactant (C) on three dependent variables, particles size (Y1), entrapment efficiency (Y2), and drug release (Y3). 3-D surface response plots were drawn and optimized formulation was selected based on desirability factor. Then it was coated with tween 80 for ease of permeability through blood brain barrier due to intact absorption of solid lipid nanoparticles. Results: The results of coated optimized formulation showed average particle size of 108.9 nm, entrapment efficiency of 78.62%, and in vitro drug release of 98.88±0.102% at 36 hr at pH 7.4. Morphologically, particles were almost spherical in shape with uniform size distribution. Targeting of coated optimized formulation to brain after oral administration was confirmed by fluorescence microscopy studies on male albino wistar strain rats. This research also envisaged that there is a >85% cell viability up to 125µg/ ml concentration of coated solid lipid nanoparticles by MTT assay. Conclusion: Thus, the current study successfully designed, developed an optimized SLN formulation of Asenapine maleate using a 3-factor, 3-level Box-Behnken design for brain targeting to treat Schizophrenia by bypassing the first pass metabolism with enhanced oral bioavailability.

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FABRICATION AND CHARACTERIZATION OF RALOXIFENE LOADED SOLID-LIPID NANOPARTICLES

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i4.41774 ◽

2021 ◽

pp. 185-191

Author(s):

NAVIN CHANDRA PANT ◽

VIJAY JUYAL

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Goodness Of Fit ◽

Water Solubility ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Poloxamer 407 ◽

Formulation Development ◽

Solid Lipid

Objective: The poor water solubility of the drug presents a great challenge for the formulation development and results in low oral bioavailability. The oral bioavailability of Raloxifene HCl (RLX) is very low (<2%) in humans due to its poor solubility. The objective of the present study was to develop RLX loaded solid-liquid nanoparticles for effective drug delivery. Methods: Compritol 888 ATO-based RLX-loaded solid lipid nanoparticles (SLNs) were formulated using the oil in water microemulsion method. Drug-excipients compatibility was confirmed through Fourier transform infrared spectroscopy, Differential scanning calorimetry methods. The SLN was characterized for particle size, surface morphology, entrapment efficiency. Results: A total of seventeen formulations (SLN1-SLN17) were developed as per the 3 levels 3 factor Box–Behnken design. The model used for the analysis was statistically analyzed using ANOVA and the goodness of fit was evaluated using diagnostic plots. As per the response-surface plots, the amount of lipid, poloxamer 407, and ultrasonication time have a significant effect on the particle size and entrapment efficiency (%EE). The developed RLX-loaded SLNs have the size and %EE in the range of 165.63±2.62 nm to 315.33±4.87 nm and 75.21±2.32% to 95.32±2.11%. The TEM analysis showed that the developed RLX-loaded SLNs were almost spherical and has a small size range. Conclusion: The high biocompatibility, biodegradability, ability to protect drugs in GIT, and sustained release properties make SLNs an ideal candidate to resolve poor oral bioavailability challenges.

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