A Novel Approach for the Development of a Nanostructured Lipid Carrier Formulation by Hot-Melt Extrusion Technology

Bhagurkar, Ajinkya M.; Repka, Michael A.; Murthy, S. Narasimha

doi:10.1016/j.xphs.2016.12.015

Cited by 51 publications

(24 citation statements)

References 25 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…HME-Us have gained a lot of importance after the Food and Drug Administration encouraged the use of continuous processes among the pharmaceutical industry [41] and overcome most of the limitations offered by the conventional microand nanoemulsification techniques. Avoidance of organic solvents, shorter and lower steps of the process as well as the increased homogeneous spreading of the particles are some of the advantages of this method [42,43]. Altogether, this makes HME-Us an industrially and environmentally friendly technique that has largely been applied in the preparation of NLCs for multiple applications [44,45].…”

Section: Resultsmentioning

confidence: 99%

Encapsulation of Oleuropein in Nanostructured Lipid Carriers: Biocompatibility and Antioxidant Efficacy in Lung Epithelial Cells

et al. 2020

View full text Add to dashboard Cite

Oxidative damage has been linked to a number of diseases. Oleuropein (OLE), a natural occurring polyphenol from olive leaves (Olea europaea L.), is known to be a potent antioxidant compound with inherent instability and compromised bioavailability. Therefore, in this work, nanostructured lipid carriers (NLCs) were proposed for OLE encapsulation to protect and improve its antioxidant efficacy. The lipid matrix, composed of olive oil and Precirol, was optimized prior to OLE encapsulation. The characterization of the optimized oleuropein-loaded NLCs (NLC-OLE) showed a mean size of 150 nm, a zeta potential of −21 mV, an encapsulation efficiency of 99.12%, sustained release profile, and improved radical scavenging activity. The cellular in vitro assays demonstrated the biocompatibility of the NLCs, which were found to improve and maintain OLE antioxidant efficacy in the A549 and CuFi-1 lung epithelial cell lines, respectively. Overall, these findings suggest a promising potential of NLC-OLE to further design a pulmonary formulation for OLE delivery in lung epithelia.

show abstract

Section: Resultsmentioning

confidence: 99%

Encapsulation of Oleuropein in Nanostructured Lipid Carriers: Biocompatibility and Antioxidant Efficacy in Lung Epithelial Cells

et al. 2020

View full text Add to dashboard Cite

show abstract

“…Solid lipid nanoparticles (SLNs) have been widely used for drug delivery via oral, topical, ophthalmic, parenteral and other routes [130][131][132][133][134][135][136][137][138][139][140][141][142]. SLNs suffer from some disadvantages such as burst release with hydrophilic drugs and low drug loading owing to the solid crystalline state of the nanoparticles.…”

Section: Solid Lipid Nanoparticlesmentioning

confidence: 99%

Recent Advances in Topical Nano drug-delivery Systems for the Anterior Ocular Segment

2018

View full text Add to dashboard Cite

Over the past decade, there has been a rise in the number of clinical cases of moderate to severe anterior segment ocular diseases. Conventional topical ophthalmic formulations have several limitations - to address which, novel drug-delivery systems are needed. Additionally, formidable physiological barriers limit ocular bioavailability through the topical route of application. During the last decade, various nano-scaled ocular drug-delivery strategies have been reported. Some of these exploratory, topical, noninvasive approaches have shown promise in improving penetration into the anterior segment tissues of the eye. In this article, we review the available literature with respect to the safety, efficiency and effectiveness of these nano systems.

show abstract

“…First developed and used in the plastics industry, hot melt extrusion (HME) has been applied in the pharmaceutical industry as a simple, reproducible, and fast method for producing many solid dosage forms of drugs [ 1 , 2 ] for different delivery routes, such as the oral route (granules, pellets, and tablets) [ 3 , 4 , 5 , 6 ], the transdermal and transmucosal route [ 7 ], and the subcutaneous route (implants) [ 8 , 9 , 10 ], some of the most widely developed applications are for: Taste masking [ 11 , 12 ] Improved dissolution of poorly soluble drugs [ 13 , 14 , 15 , 16 ] Sustained release formulations [ 17 , 18 ] and Preparation of nanosystems [ 19 , 20 , 21 , 22 ]. …”

Section: Introductionmentioning

confidence: 99%

Hot Melt Extrusion: Highlighting Physicochemical Factors to Be Investigated While Designing and Optimizing a Hot Melt Extrusion Process

et al. 2018

View full text Add to dashboard Cite

Hot-melt extrusion (HME) is a well-accepted and extensively studied method for preparing numerous types of drug delivery systems and dosage forms. It offers several advantages: no solvents are required, it is easy to scale up and employ on the industrial level, and, in particular, it offers the possibility of improving drug bioavailability. HME involves the mixing of a drug with one or more excipients, in general polymers and even plasticizers, which can melt, often forming a solid dispersion of the drug in the polymer. The molten mass is extruded and cooled, giving rise to a solid material with designed properties. This process, which can be realized using different kinds of special equipment, may involve modifications in the drug physicochemical properties, such as chemical, thermal and mechanical characteristics thus affecting the drug physicochemical stability and bioavailability. During process optimization, the evaluation of the drug solid state and stability is thus of paramount importance to guarantee stable drug properties for the duration of the drug product shelf life. This manuscript reviews the most important physicochemical factors that should be investigated while designing and optimizing a hot melt extrusion process, and by extension, during the different pre-formulation, formulation and process, and post-formulation phases. It offers a comprehensive evaluation of the chemical and thermal stability of extrudates, the solid physical state of extrudates, possible drug-polymer interactions, the miscibility/solubility of the drug-polymer system, the rheological properties of extrudates, the physicomechanical properties of films produced by hot melt extrusion, and drug particle dissolution from extrudates. It draws upon the last ten years of research, extending inquiry as broadly as possible.

show abstract

A Novel Approach for the Development of a Nanostructured Lipid Carrier Formulation by Hot-Melt Extrusion Technology

Cited by 51 publications

References 25 publications

Encapsulation of Oleuropein in Nanostructured Lipid Carriers: Biocompatibility and Antioxidant Efficacy in Lung Epithelial Cells

Encapsulation of Oleuropein in Nanostructured Lipid Carriers: Biocompatibility and Antioxidant Efficacy in Lung Epithelial Cells

Recent Advances in Topical Nano drug-delivery Systems for the Anterior Ocular Segment

Hot Melt Extrusion: Highlighting Physicochemical Factors to Be Investigated While Designing and Optimizing a Hot Melt Extrusion Process

Contact Info

Product

Resources

About