scholarly journals Invivo Pharmacokientic and Pharamacodynamic Studies of Optimized Antihyperlipidemic Drug Loaded Solid Lipid Nanoparticle

2020 ◽  
Vol 11 (4) ◽  
pp. 7454-7463
Author(s):  
Gannimani Veerabhadra Rao ◽  
Gadela Venkata Radha ◽  
Krishnaji Rao M ◽  
Brito Raj S ◽  
Bhaskar Reddy K
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Therapeutic Response ◽  
Drug Carrier ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Carrier Mechanism ◽  
The Stability ◽  
Evaluation Parameters

The purpose of this research is to increase bioavailability by solid lipid nanoparticle (SLN) carrier for low bioavailable drugs (< 5%) such as Lovastatin. Eight SLN loaded Lovastatin was designed and optimised by variables such as Particle Size (PS in nm) and Zeta Potential (ZP in mV) using a micro emulsification technique. SLN 7 was chosen as the optimised formulation according to the findings obtained and the same was chosen for invivo pharmacokinetic and triton-induced antihyperlipidemic operation. SLN7 confirms an improvement in bioavailability of 3.15 percent by an improvement in AUC compared to conventional dosage type (Altoprev) from the pharmacokinetic invivo results. SLN was also an appropriate career in drug delivery for Lovastatin by enhancing bioavailability and therapeutic response. The stability studies of SLN7 revealed that the evaluation parameters of SLN did not change significantly. It was verified from the data that the drug-loaded SLN was stable under varying temperature and humidity conditions. While compare to 25˚c±2˚c/ 60% RH, SLN are more stable in 4˚c±2˚c  and shows good reproducible reports in Particle Size (nm), Zeta potential (mV), PI and EE% data. Therefore, Solid Lipid Nanoparticle is a viable drug carrier mechanism for low bioavailable Lovastatin to improve their bioavailability through efficiently permeating them.

scholarly journals α-GLUCOSIDASE INHIBITORY ACTIVITY AND FORMULATION OF SOLID LIPID NANOPARTICLE CONTAINING ETHANOL 70% STANDARDIZED EXTRACT OF KUMIS KUCING LEAVES (Orthosiphon stamineus Benth.)

2018 ◽  
Vol 16 (1) ◽  
pp. 45
Author(s):  
Risma Marisi Tambunan ◽  
Winda Dwi Juliyanti
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Data Processing ◽  
Inhibitory Activity ◽  
Tween 80 ◽  
Solid Lipid Nanoparticle ◽  
Orthosiphon Stamineus ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Significant Difference

Kumis kucing leaves (Orthosiphon stamineus Benth.) are one type of plants that is able to inhibit the activity of α-glucosidase enzyme. This study aims to formulate Solid Lipid Nanoparticle from ethanol 70% standardized extract of kumis kucing leaves and which give α-glucosidase enzyme inhibitory activity. The result of SLN characteristic for particle size of formula I, II and III shows the result of 51,60 nm; 12.81 nm; 11.87 nm and zeta potential of formula I, II and III show the results -27.67; -10,7; -15.0, respectively. The results of the α-glucosidase enzyme inhibitory activity of the standardized extract, SLN formula I, II and III respectively showed IC50 of 132.9 ppm; 130.3 ppm; 131.4 ppm; 132.2 ppm and Acarbose as comparison showed IC50 of 50.0 ppm. Data processing using t-test statistically at α = 0,05 showed that extract and SLN of formula I had significant difference, thus the best SLN formula was formula I with concentration of tween 80 and propylenglycol of 6% and 10%.

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

2019 ◽  
Vol 9 (3) ◽  
pp. 212-221 ◽  
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

scholarly journals Pengembangan Formula Solid Lipid Nanoparticles (SLN) Hidrokortison Asetat

2019 ◽  
Vol 6 (1) ◽  
pp. 83
Author(s):  
Garnadi Jafar ◽  
Eriska Agustin ◽  
Deny Puryani
Keyword(s):  
Particle Size ◽  
Loading Capacity ◽  
Hydrocortisone Acetate ◽  
Solid Lipid Nanoparticle ◽  
Inflammatory Skin Disease ◽  
Disease Treatment ◽  
Solid Lipid ◽  
Magnetic Stirrer ◽  
Lipid Nanoparticle ◽  
Capacity Method

ABSTRAK             Dermatitis Atopik (DA) adalah penyakit inflamasi kulit kronis dan kambuhan, terutama pada anak-anak. Pengobatan DA salah satunya menggunakan hidrokortison. Sifat lipofil dari hidrokortison asetat (HA) akan berpengaruh terhadap penetrasinya kedalam kulit jika diberikan secara topikal. SLN (Solid Lipid Nanoparticle) merupakan sistem penghantaran obat baru yang terdiri dari matriks lipid padat dan surfaktan yang terdispersi dalam air dengan ukuran partikel 10-1000nm untuk meningkatkan solubility, stability, dan loading capacity. Metode: SLN dibuat dengan homogenisasi panas menggunakan magnetic stirrer selama 10 menit suhu 600C, dilanjutkan dengan ultraturax 5000rpm selama 10 menit dan ultrasonikasi dengan sonikator probe dengan amplitudo 55% selama 15 menit, mode pulse on-off 10 detik. Optimasi basis SLN dilakukan pada beberapa jenis lipid (GMS Cutina dan Apifil) dan surfaktan (Pluracare, Tegocare, Plantacare, dan Cremofor RH 40). Basis SLN yang terpilih adalah GMS Cutina sebagai lipid padat dengan kosentrasi 4%,5%, dan 6% dan surfaktan Pluracare 3% berdasarkan ukuran partikel terkecil, FTIR, dan DSC yang menunjukkan kompatibilitas dengan HA. Hasil: Formula SLN hidrokortison asetat yang digunakan adalah lipid padat GMS Cutina 4%-6% dan surfaktan Pluracare 3% menghasilkan ukuran partikel 806nm ± 124,67nm - 958nm ± 91,28nm, nilai PI masing-masing 0,874±0,07 - 0,943±0,15, dan nilai efisiensi penjerapan (EE) 12,5%, - 83,3%. Kata Kunci : Hidrokortison Asetat, Homogenisasi Panas, SLN (Solid Lipid Nanoparticle), Ultrasonikasi ABSTRACT Atopic dermatitis (DA) is a recurrent chronic inflammatory skin disease. Treatment of DA used one of them is hydrocortisone acetate. The lipophilic properties of hydrocortisone acetate (HA) will affect its penetration into the skin when administered topically. SLN (Solid Lipid Nanoparticle) is a new drug delivery system consisting of a solid lipid matrix and a water dispersed surfactant with a particle size of 10-1000nm to improve solubility, stability, and loading capacity. Method: SLN used hot homogenization using magnetic stirrer for 10 minutes temperature 600C, followed by ultraturax 5000rpm for 10 minutes and ultrasound with probe sonicator with 55% amplitude for 15 minutes, 10 second pulse on-off mode. Optimization of the SLN base was performed on several types of lipids (GMS Cutina and Apifil) and surfactants (Pluracare, Tegocare, Plantacare, and Cremofor RH 40). The preferred SLN base is GMS Cutina as a solid lipid with a concentration of 4%, 5%, and 6% and a 3% Pluracare as a surfactant based on the smallest particle size, FTIR, and DSC showing compatibility with HA. Result: The formula of SLN hydrocortisone acetate used GMS Cutina 4% -6% as a solid lipid and Pluracare 3% as a surfactant resulted a particle size of 806nm ± 124.67nm - 958nm ± 91.28nm, PI value of 0.874 ± 0.07 - 0.943 ± 0.15 , and the efficiency entrapment (EE) 12.5%, - 83.3%. Keywords : Hydrocortisone Acetate, Hot Homogenization, SLN (Solid Lipid Nanoparticle), Ultrasound

scholarly journals Formulation and evaluation of prazosin hydrochloride loaded solid lipid nanoparticles

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

scholarly journals Development and Optimization of Solid Lipid Nanoparticle for Topical Delivery

2019 ◽  
Vol 9 (5-s) ◽  
pp. 105-121
Author(s):  
Pallavi M Chaudhari ◽  
Mahananda.V Ghodake
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Solid Lipid Nanoparticle ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Solid Lipid ◽  
Lipid Nanoparticle

The aim of present work was to develop and evaluate solid lipid nanoparticle (SLNs) based gel for topical delivery of anti-inflammatory drug. Material and method Nabumetone loaded SLNs were developed by hot homogenization followed by ultra- sonication technique using compritol 888 ATO as solid lipid and tween 80 as a surfactant. Developed SLNs were evaluated for particle size, entrapment efficiency (EE) and drug release profile. Process and formulation parameters were optimized. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies were carried out on SLNs to mark the change in the drug and lipid modification. The Nabumetone based gels were prepared using carbopol 940 as gelling agent. Results and conclusion: The F14 batch had shown maximum entrapment efficiency up to 94.40 and sustained drug release for more than 7 hours. The particle size of optimized batch (F14) was found to be 16.54. Keywords: Solid lipid nanoparticle, Entrapment efficiency, Colloidal carrier.

Development & Pharmaceutical Characterization of Isoniazid Loaded Solid Lipid Nanoparticle Drug Delivery Approach

2019 ◽  
Vol 14 (3) ◽  
pp. 228-238
Author(s):  
Swatantra Kumar Singh Kushwaha ◽  
Awani Kumar Rai ◽  
Heena Parveen
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Diffusion Mechanism ◽  
Antitubercular Drug ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Background: Tuberculosis is a major public health problem in the world. Isoniazid is a first line antitubercular drug active against Mycobacterium species which inhibits mycolic acid synthesis. Objective: The aim of the present investigation was the preparation of solid lipid nanoparticle containing Isoniazid to increase bioavailability, sustained release and decrease toxicity by increasing permeability. Methods: Isoniazid was incorporated into SLN for sustained drug delivery, increasing permeability and bioavailability. SLNs were prepared by emulsification followed by the solvent evaporation technique by optimizing lipid, polymer and surfactant ratio under controlled optimized process variables i.e. temperature and stirring speed. SLNs were characterized for particle size analysis, comparative study design in different physiological pH for in-vitro drug release and drug release kinetics. Results: The best in-vitro release for F7 was found to be 80.2% in pH-7.4 and 82.2% in pH-4.5. The particle size of the F7 formulation was found to be in the range of 200- 600nm . Among all 3 optimized formulations, i.e. F3, F7 and F8 in both the pH, F3 followed non-fickian diffusion mechanism in pH-4.5 whereas all the formulations in both pH followed super-case II diffusion mechanism. The stability studies were carried out as per ICH guidelines which signify that the SLNs were found stable in the refrigerated condition. Conclusion: The results clearly demonstrated that SLNs drug delivery system is a promising approach for antitubercular drug delivery as it proved to sustained release, increase permeability, enhanced bioavailability and thus decreased dosing frequency. Kinetic modelling of the formulation with zero, first order, Higuchi and Korsmeyer- peppas is explained in this article.

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