scholarly journals Solid lipid nanocarriers as alternative drug delivery system for improved oral delivery of drugs

2020 ◽  
Vol 10 (6-s) ◽  
pp. 168-172
Author(s):  
Gorre Thirupathi ◽  
Samanthula Kumara Swamy ◽  
Alli Ramesh
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Lipid Nanoparticles ◽  
Delivery Systems ◽  
Chemical Degradation ◽  
Solid Lipid ◽  
First Pass Metabolism ◽  
First Pass ◽  
Lipid Nanocarriers ◽  
Pass Metabolism

Oral bioavailability of drugs is mainly limited due to the poor aqueous solubility, enhanced chemical degradation, reduced permeation and/or first pass metabolism. Various novel delivery systems are developed for improved oral bioavailability of these drugs such as modified orals, buccal, transdermal and osmotic delivery systems. Colloidal carrier systems such as nanoparticles, lipid nanoparticles, nanoemulsions, microspheres, liposomes, resealed erythrocytes and transfersomes were also developed to enhance the oral delivery. Among these, solid lipid nanocarriers (SLNs) also gain much attention on the enhancement of oral bioavailability. SLNs are submicron sized nanoparticles and composed of solid lipid, surfactants and cosurfactants. The enhanced oral bioavailability of poorly soluble drugs from SLNs might be due to the reduced particle size, bypassed presystemic metabolism, and enhanced gastric mucosa permeability. Vast literature is available for the advantages, limitations, preparation methods, evaluation parameters and application of SLNs in different routes. This review mainly focused on list of drugs developed as SLNs and considered as an alternative approach to enhance the oral bioavailability based on pharmacokinetic as well as pharmacodyanmic parameters was discussed. Keywords: Oral bioavailability, solubility, first-pass metabolism, solid lipid nanoparticles, pharmacokinetics, pharmacodynamics.

Development and Optimization of Mirabegron of Solid Lipid Nanoparticles as an Oral Delivery for Overactive Bladder

2021 ◽  
Vol 09 ◽  
Author(s):  
Prajakta Raut ◽  
Makarand Gambhire ◽  
Dhruvi Panchal ◽  
Vaishali Gambhire
Keyword(s):  
Overactive Bladder ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Lipid Nanoparticles ◽  
Correlation Spectroscopy ◽  
Solid Lipid ◽  
Peg 400 ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Background: Mirabegron (MBN), a β-3 adrenergic agent, is used in the treatment of overactive bladder. MBN has alow water solubility, high first-pass metabolism, and low bioavailability, consequently, having poor absorption in the gastrointestinal tract. Objective: The present study is intended at formulating Mirabegron-loaded solid lipid nanoparticles (MBN-SLN) coated with PEG-400 to bypass hepatic first-pass metabolism and to improve its oral bioavailability. Methods: MBN-SLNs were developed using glyceryl monostearate by pre-emulsion- ultrasonication method which was then optimized applying Box-Behnken Design. The optimized batch of MBN-SLN was selected for surface-modification with PEG-400 (MBN-PEG-SLN) and characterized by photon correlation spectroscopy, DSC, and XRD. Bioavailability studies were conducted in Wistar rats after oral administration of plain MBN dispersion, MBN-SLN, and MBN-PEG-SLN. Results: Stable MBN-SLNs and MBN-PEG-SLN of the optimized batch having a mean particle size of 162.7 nm and 149.9 nm; Zeta potential of -39.1 mV and -30.9 mV; %entrapment of 89.90% and 90.12%, respectively, were developed. The results of the in-vitro drug release studies demonstrated a significant slow release of MBN from MBN-SLN (69.38%) and MBN-PEG-SLN (61.33%) as compared to the dispersion of pure drug (92.10%). The relative bioavailability, as a result of the invivostudies, of MBN from MBN-PEG-SLN increased by 2-fold, based on the Cmax values, in comparison with the plain MBN dispersion. Conclusion: Thus, the study established that the oral bioavailability of MBN could be improved by the administration of MBN-PEG-SLN. The obtained results indicate SLNs as a potential drug delivery system for improving the bioavailability of poorly bioavailable drugs such as MBN by abating the first-pass metabolism.

scholarly journals Preparation, Characterization and Evaluation of Quetiapine Fumarate Solid Lipid Nanoparticles to Improve the Oral Bioavailability

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Arjun Narala ◽  
Kishan Veerabrahma
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Scanning Calorimetry ◽  
Quetiapine Fumarate ◽  
Solid Lipid ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Quetiapine fumarate is an antipsychotic drug with poor oral bioavailability (9%) due to first-pass metabolism. Present work is an attempt to improve oral bioavailability of quetiapine fumarate by incorporating in solid lipid nanoparticles (SLN). Six quetiapine fumarate SLN formulations were developed using three different lipids by hot homogenisation followed by ultrasonication. The drug excipient compatibility was studied by differential scanning calorimetry (DSC). Stable quetiapine fumarate SLNs having a mean particle size of 200–250 nm with entrapment efficiency varying in between 80% and 92% were developed. The physical stability of optimized formulation F3 was checked at room temperature for 2 months. Comparative bioavailability studies were conducted in male Wistar rats after oral administration of quetiapine fumarate suspension and SLN formulation. The relative bioavailability of quetiapine fumarate from optimized SLN preparation was increased by 3.71 times when compared with the reference quetiapine fumarate suspension. The obtained results are indicative of SLNs as potential lipid carriers for improving the bioavailability of quetiapine fumarate by minimizing first-pass metabolism.

Development of Lipid-Based Nanocarriers for Increasing Gastrointestinal Absorption of Lupinifolin

Planta Medica ◽  
2020 ◽  
Vol 86 (05) ◽  
pp. 364-372 ◽  
Author(s):  
Jidapa Musika ◽  
Nuannoi Chudapongse
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Medium Chain Triglyceride ◽  
Lipid Nanoparticles ◽  
Delivery Systems ◽  
Nanostructured Lipid Carriers ◽  
Gastrointestinal Absorption ◽  
Prolonged Release ◽  
Solid Lipid ◽  
Lipid Nanocarriers

AbstractLupinifolin, a plant flavonoid, has been reported to possess various pharmacological effects. It most likely exerts low oral bioavailability because of poor water solubility. The objective of this study was to develop lipid nanocarriers as drug delivery systems to increase the gastrointestinal absorption of lupinifolin extracted from Albizia myriophylla. Three types of nanocarriers, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were prepared by an emulsification-sonication technique. All three types of nanocarriers loaded with lupinifolin, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were successfully synthesized. The lipid components chosen to formulate nanocarriers were tripalmitin and/or medium chain triglyceride. Physicochemical characterizations along with releasing profiles of lupinifolin-loaded lipid nanocarriers were compared. It was found that the best lipid nanocarrier for lupinifolin was lupinifolin-loaded nanostructured lipid carriers, which demonstrated the particle size of 151.5 ± 0.1 nm, monodispersity distribution with a polydispersity index of 0.24, negative surface charge at − 41.2 ± 0.7 mV, high encapsulation (99.3%), and high loading capacity (5.0%). The obtained lupinifolin-loaded nanostructured lipid carriers exhibited prolonged release in a simulated circulatory system but produced a low release in gastrointestinal conditions (3.7%). Intestinal permeability of the nanocarriers was further evaluated in everted intestinal sacs. The results from the ex vivo study indicated that lupinifolin-loaded nanostructured lipid carriers significantly increased the absorption of lupinifolin compared to the native form. In conclusion, lupinifolin-loaded lipid nanocarriers were successfully formulated as delivery systems to enhance its oral bioavailability. Further in vivo experiments are needed to validate the results from this study.

scholarly journals Quality by Design Approach for Development and Characterisation of Solid Lipid Nanoparticles of Quetiapine Fumarate

2020 ◽  
Vol 16 (1) ◽  
pp. 73-91 ◽  
Author(s):  
Shweta Agarwal ◽  
Rayasa S. Ramachandra Murthy ◽  
Sasidharan Leelakumari Harikumar ◽  
Rajeev Garg
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Quality By Design ◽  
Lipid Nanoparticles ◽  
Lymphatic Transport ◽  
Quetiapine Fumarate ◽  
Solid Lipid ◽  
First Pass Metabolism ◽  
First Pass ◽  
Quality By Design Approach ◽  
Pass Metabolism

Background: Quetiapine fumarate, a 2nd generation anti-psychotic drug has oral bioavailability of 9% because of hepatic first pass metabolism. Reports suggest that co-administration of drugs with lipids affects their absorption pathways, enhances lymphatic transport thus bypassing hepatic first-pass metabolism resulting in enhanced bioavailability. Objective: The present work aimed at developing, and characterising potentially lymphatic absorbable Solid Lipid Nanoparticles (SLN) of quetiapine fumarate by Quality by Design approach. Method: Hot emulsification followed by ultrasonication was used as a method of preparation. Precirol ATO5, Phospholipon 90G and Poloxamer 188 were used as a lipid, stabilizer and surfactant respectively. A32 Central Composite design optimised the 2 independent variables, lipid concentration and stabilizer concentration and assessed their effect on percent Entrapment Efficiency (%EE: Y1). The lyophilized SLNs were studied for stability at 5 ±3οC and 25 ± 2οC/60 ± 5% RH for 3 months. Results: The optimised formula derived for SLN had 270mg Precirol ATO5 and 107mg of Phospholipon 90G giving %EE of 76.53%. Mean particle size was 159.8nm with polydispersity index 0.273 and zeta potential -6.6mV. In-vitro drug release followed Korsmeyer-Peppas kinetics (R2=0.917) with release exponent n=0.722 indicating non-Fickian diffusion. Transmission electron microscopy images exhibited particles to be spherical and smooth. Fourier-transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction studies ascertained drug-excipient compatibility. Stability studies suggested 5οC as appropriate temperature for storage and preserving important characteristics within acceptable limits. Conclusion: Development and optimisation by Quality by Design were justified as it yielded SLN having acceptable characteristics and potential application for intestinal lymphatic transport.

scholarly journals Transmucosal Solid Lipid Nanoparticles to Improve Genistein Absorption via Intestinal Lymphatic Transport

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 267
Author(s):  
Antonella Obinu ◽  
Giovanni Pietro Burrai ◽  
Roberta Cavalli ◽  
Grazia Galleri ◽  
Rossana Migheli ◽  
...  
Keyword(s):  
Intestinal Mucosa ◽  
Solid Lipid Nanoparticles ◽  
Biological Effects ◽  
Lipid Nanoparticles ◽  
Neuroprotective Activity ◽  
Testing Time ◽  
Solid Lipid ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Genistein (GEN) is a soy-derived isoflavone that exhibits several biological effects, such as neuroprotective activity and the prevention of several types of cancer and cardiovascular disease. However, due to its poor water solubility and the extensive first-pass metabolism, the oral bioavailability of GEN is limited. In this work, solid lipid nanoparticles (SLN) were developed to preferentially reach the intestinal lymphatic vessels, avoiding the first-pass metabolism of GEN. GEN-loaded SLN were obtained by a hot homogenization process, and the formulation parameters were chosen based on already formulated studies. The nanoparticles were characterized, and the preliminary in vitro chylomicron formation was evaluated. The cell uptake of selected nanocarriers was studied on the Caco-2 cell line and intestinal mucosa. The SLN, characterized by a spherical shape, showed an average diameter (about 280 nm) suitable for an intestinal lymphatic uptake, good stability during the testing time, and high drug loading capacity. Furthermore, the intestinal mucosa and Caco-2 cells were found to uptake SLN. The approximately two-fold increase in particle size suggested a possible interaction between SLN and the lipid components of chylomicrons like phospholipid; therefore, the results may support the potential for these SLN to improve oral GEN bioavailability via intestinal lymphatic absorption.

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 Lipid-based nanocarriers for oral delivery of peptides

OCL ◽  
2022 ◽  
Vol 29 ◽  
pp. 1
Author(s):  
Camille Dumont
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Intestinal Transport ◽  
Intestinal Lumen ◽  
Burst Release ◽  
Solid Lipid ◽  
Lipid Nanocarriers ◽  
Therapeutic Peptides ◽  
Poor Stability ◽  
Platelet Shape

Therapeutic peptides can treat a wide variety of diseases with selective and potent action. Their oral bioavailability is strongly limited by an important proteolytic activity in the intestinal lumen and poor permeation across the intestinal border. We have evaluated the capacity of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) to overcome both oral bioavailability limiting aspects, using leuprolide (LEU) as model peptide. Lipidization of LEU by formation of a hydrophobic ion pair (HIP) with sodium docusate enables a significant increase of peptide encapsulation efficiency in both SLN and NLC. The nanocarriers, obtained by high-pressure homogenization, measured 120 nm and were platelet shaped. Regarding the protective effect towards proteolytic degradation, only NLC maintained LEU integrity in presence of trypsin. Intestinal transport, evaluated on Caco-2 (enterocyte-like model) and Caco-2/HT29-MTX (mucin-secreting model) monolayers, showed nanocarriers internalization by enterocytes but no improvement of LEU permeability. Indeed, the combination of nanoparticles platelet-shape with the poor stability of the HIP in the transport medium induces a high burst release of the peptide, limiting nanoparticles capacity to transport LEU across the intestinal border. Stability of peptide lipidization needs to be improved to withstand biorelevant medium to benefit from the advantages of encapsulation in solid lipid nanocarriers and consequently improve their oral bioavailability.

scholarly journals Oral dissolving film: present and future aspects

2018 ◽  
Vol 8 (6) ◽  
pp. 373-377
Author(s):  
Prabhjot Kaur ◽  
Rajeev Garg
Keyword(s):  
Thin Film ◽  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Innovative Drug ◽  
Patient Acceptability ◽  
First Pass Metabolism ◽  
First Pass ◽  
Recent Trends ◽  
Pass Metabolism

Over the past few decades, tendency toward innovative drug delivery systems has almightily increased attempts to ensure efficacy, safety and patient acceptability. As discovery and development of new chemical agents is a complex, expensive and time consuming process, so recent trends are shifting toward designing and developing innovative drug delivery systems for existing drugs. Orally fast dissolving film is the kind of drug delivery system which when placed in the oral cavity, disintegrate or dissolve within a few seconds without the intake of water. Oral fast dissolving film is relatively new dosage form in which thin film is prepared using hydrophilic polymers, which rapidly disintegrate or dissolves on tongue or in the buccal cavity It is an alternative platform for molecules that undergoes high first pass metabolism. The method of preparation for oral dissolving film. Solvent casting, Semisolid casting, Hot melt extrusion, Solid dispersion extrusion, Rolling The current evaluation gives an account of different formulations methods of preparation and quality control of the fast dissolving oral thin film. Keyword:  First pass metabolism, Tensile strength,  Fast Dissolving Oral Film etc.

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