Lipid-Based Nanocarriers for Oral Delivery of Proteins and Peptides: Opportunities, Challenges, and Future Prospects (original) (raw)
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Nanostructured Lipid Carriers for Improved Delivery of Therapeutics via the Oral Route
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Drug delivery via the oral route has always been challenging for poorly soluble drugs. Acid-induced hydrolysis, enzymatic degradation, and poor mucosal absorbency remain the primary hiccups for effective oral delivery of medications. With the advent of nanotechnology, nanostructured lipid carriers (NLCs) have emerged as a promising delivery carrier that can circumvent gastrointestinal tract (GIT) barriers hindering the solubility and bioavailability of such drugs. These NLCs can efficiently transport drug moieties across intestinal membranes shielding medications from intestinal pH and enzymatic degradation. Because they are composed of lipidic materials, they can be easily absorbed or taken up by various pathways such as transcellular absorption, paracellular transport, and M-cell uptake. Such mechanisms not only improve the absorption and solubility of drugs but also augment bioavailability and residence time and may bypass first-pass metabolism. This review explores the diverse a...
Nanostructured lipid carriers: A platform to lipophilic drug for oral bioavailability enhancement
Journal of Drug Delivery and Therapeutics, 2019
Lipid based drug delivery system such as Solid lipid nanoparticle (SLN) and Nanostructured lipid carriers (NLC) are among the most promising drug delivery system used in many industries such as food, pharmaceuticals and cosmetics industries. Over the last few years, new constituents of lipids have developed and investigated for enhancement of bioavailability. The present manuscript is an attempt on solving the concerned uncertainty with efficacious peroral administration of hydrophobic drugs through fabricating new lipid formulations, NLC. NLC, the secondgeneration lipid carrier is usually composed of solid lipids and liquid lipids together in a system. This mixing causes depression in melting point of substrates and converts the mixture into solid form at body temperature and termed as NLC. NLC shows a high drug loading with minimum drug expulsion. The unique advantages of NLC over SLN and Lipid-drug conjugates (LDC) are increased capacity of drug loading, avoidance of drug expulsion. This manuscript gives detailed information on definitions and simple way of production methods, new approaches in formulation of NLC and it also highlights how NLC improves bioavailability of bioactive molecules through peroral route and its future perspective as a pharmaceutical carrier. It also gives idea about the supremacy of NLC over other lipid-based system.
Nanostructured lipid carriers: versatile oral delivery vehicle
Oral delivery is the most accepted and economical route for drug administration and leads to substantial reduction in dosing frequency. However, this route still remains a challenge for the pharmaceutical industry due to poorly soluble and permeable drugs leading to poor oral bioavailability. Incorporating bioactives into nanostructured lipid carriers (NLCs) has helped in boosting their therapeutic functionality and prolonged release from these carrier systems thus providing improved pharmacokinetic parameters. The present review provides an overview of noteworthy studies reporting impending benefits of NLCs in oral delivery and highlights recent advancements for developing engineered NLCs either by conjugating polymers over their surface or modifying their charge to overcome the mucosal barrier of GI tract for active transport across intestinal membrane. Lay abstract: Oral administration of drugs is considered to be a convenient route; however, various drugs that are insoluble in water or unable to permeate across GI tract membrane cannot be delivered by this route. To deliver them effectively, various lipid carriers have been widely explored by researchers. Lipid carriers encapsulate drug inside them and deliver them effectively via the oral route. Also, encapsulation of drug protects them from degradation inside GI tract and safely delivers them to the site of action. This review summarizes application of lipid carriers, in other words, nanostructured lipid carriers, in eradicating these problems, with suitable examples.
International journal of pharmaceutical investigation
Nowadays exploration of novel lipid-based formulations is akin to a magnet for researchers worldwide for improving the in vivo performance of highly lipophilic drugs. Over the last few years, new compositions of lipids have been developed, and the probable bioavailability enhancement has been investigated. We reviewed the most recent data dealing with backlogs of conventional lipid-based formulations such as physical instability, limited drug loading capacities, drug expulsion during storage along with all the possible hindrances resulting in poor absorption of highly lipophilic drugs such as P-glycoprotein efflux, extensive metabolism by cytochrome P450 etc. In tandem with these aspects, an exclusive formulation approach has been discussed in detail in this paper. Therefore, this review focuses on resolving the concerned ambiguity with successful oral administration of highly lipophilic drugs through designing novel lipidic formulations (nanostructured lipid carriers [NLC]) that co...
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V, 2014
Designing feasible and effective peptide ligand modified solid lipid nanoparticles (SLNs) to improve oral bioavailability of protein drugs and evaluating the influence of mucus remains important. In the present work, two kinds of peptide ligand modified SLNs loaded with salmon calcitonin (sCT), namely, sCT CSK-SLNs and sCT IRQ-SLNs, were prepared by coupling the peptide ligand CSKSSDYQC (CSK) which was reported to show affinity with goblet cells, or IRQRRRR (IRQ), a cell penetrating peptide, to polyoxyethylene (40) stearate (SA-PEG2000). Compared with unmodified SLNs, CSK or IRQ modified SLNs with better drug protection ability could facilitate the internalization of drug on Caco-2/HT29-MTX co-cultured cells and permeation in excised rat duodenum mucosa. The internalization mechanism of two kinds of peptide ligand modified SLNs was mainly active transport via both clathrin- and caveolae-dependent endocytosis. Although mucus was an impediment to the transport of SLNs, the peptide lig...
Oral drug delivery has always been considered the preferred route of drug administration. Nano-formulations are now constantly being researched for better absorption, higher bioavailability and greater therapeutic efficacy. Lipid based nanoformulations have found much favour with the formulation scientist due to their relatively higher safety profile and enhancement of bioavailability. These delivery systems are also able to protect the bioactives or drugs from the vagaries of the gastrointestinal tract. They also aid in the absorption of hydrophobic drugs which are entrapped in lipid matrices. Lipid excipients have been known to reduce efflux which is P-glycoprotein mediated and also to increase the bioavailability of bioactives which are given through the oral route.
Biomedical Materials & Devices
Low-oral bioavailability as a consequence of low-water solubility of drugs is challenging for formulation scientists in the development of new pharmaceutical products. This review aims to highlight relevant considerations when implementing a rational strategy for the development of lipid-based oral drug delivery systems and to discuss shortcomings and challenges to the current classification of these delivery systems such as nanoemulsion, Solid lipid nanoparticle (SLN), Nanostructured lipid carriers (NLC), Self-emulsifying drug delivery system (SEDDS). Lipid-based drug delivery systems consist of a diverse group of formulations, each consisting of varying functional and structural properties that are amenable to modifications achieved by varying the composition of lipid excipients and other additives thereby facilitating the bioavailability of poorly water-soluble drugs. In addition, lipid nanoparticles may also protect the loaded drugs from chemical and enzymatic degradation and gradually release drug molecules from the lipid matrix into the blood, resulting in improved therapeutic profiles compared to free drugs. Therefore, due to their physiological and biodegradable properties, lipid molecules may decrease adverse side effects and chronic toxicity of the drug-delivery systems when compared to others of polymeric nature. Accordingly, the present review is mainly centred on the various lipid-based drug delivery system and excipients used in lipid-based drug delivery systems (LBDDS).
Nanostructured Lipid Carriers: An Excellent Tool for Drug Delivery
Nanocarriers present a great approach in drug delivery. Nanostructured lipid carriers (NLCs) are a recent approach for the delivery of poorly soluble drugs with low oral bioavailability. Nanostructured Lipid Carriers (NLCs) are mixture of solid lipids along with spatially incompatible liquid lipids. It remains solid at room temperature. It also overcomes the disadvantages of various lipid particulate carriers. The present review gives insights on the definitions and characterization of NLC as colloidal carriers including the production techniques.
Review On Lipid Based Carrier As A Drug Delivery System
International Journal in Pharmaceutical Sciences, 2023
Lipid nanocarriers represent an alternative to polymeric nanoparticles, liposomes, and emulsions. Nanostructured Lipid Nanocarriers (NLCs), considered as the second-generation lipid carriers, aim to address the limitations of Solid Lipid Nanoparticles. They are employed across diverse therapeutic approaches and were initially designed for delivering lipophilic drugs, but their effectiveness with hydrophilic drugs is now well-established. The biocompatibility of lipids underpins their emergence as a promising avenue for drug delivery, exhibiting superior traits compared to other lipid formulations. This article delves into NLCs, covering their structures, preparation methods, characterization, stability, and advantages over first-generation lipid nanoparticles. The review predominantly highlights the manifold therapeutic applications of NLCs and their specificity concerning various physiological contexts. Given their biologically benign, non-immunogenic, and harmonious traits, NLCs are poised to become extensively explored systems among lipid nanocarriers.