Overview on Lipid-based Nanoparticles: Preparations, Characterizations, and Properties (original) (raw)
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Lipid Nanoparticles: Effect on Bioavailability and Pharmacokinetic Changes
The main aim of pharmaceutical technology research is the design of successful formulations for effective therapy, taking into account several issues including therapeutic requirements and patient compliance. In this regard, several achievements have been reported with colloidal carriers, in particular with lipid nanoparticles, due to their unique physicochemical properties. For several years these carriers have been showing potential success for several administration routes, namely oral, dermal, parenteral, and, more recently, for pulmonary and brain targeting. The present chapter provides a review of the use of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) to modify the release profile and the pharmacokinetic parameters of active pharmaceutical ingredients (APIs) incorporated in these lipid matrices, aiming to modify the API bioavailability, either upwards or downwards depending on the therapeutic requirement. Definitions of the morphological characteristics, surface properties, and polymorphic structures will also be given, emphasizing their influence on the incorporation parameters of the API, such as yield of production, loading capacity, and encapsulation efficiency.
Improvement of drug safety by the use of lipid-based nanocarriers
Journal of Controlled Release, 2012
Drug toxicity is an important factor that contributes significantly to adverse drug events in current healthcare practice. Application of lipid-based nanocarriers in drug formulation is one approach to improve drug safety. Lipid-based delivery systems include micelles, liposomes, solid lipid nanoparticles, nanoemulsions and nanosuspensions. These carriers are generally composed of physiological lipids welltolerated by human body. Delivery of water-insoluble drugs in these formulations increases their solubility and stability in aqueous media and eliminates the need for toxic co-solvents or pH adjustment to solubilize hydrophobic drugs. Association or encapsulation of peptides/proteins within lipid-based carriers protects the labile biologics against enzymatic degradation, hence reducing the therapeutic dose required and risk of dose-dependent toxicity. Most importantly, lipid-based nanocarriers alter the pharmacokinetics and biodistribution of drugs through passive and active targeting, leading to increased drug accumulation at target sites while significantly decreasing non-specific distribution to other tissues. Furthermore, surface modification of these nanocarriers reduces immunogenicity of drug-carrier complexes, imparts stealth by preventing opsonization and removal by phagocytes and minimizes interaction with circulating blood components. In view of heightening attention on drug safety in patient treatment, lipid-based nanocarrier is therefore an important and promising option for formulation of pharmaceutical products to improve treatment safety and efficacy.
Lipid-Based Nanoparticles as Pharmaceutical Drug Carriers: From Concepts to Clinic
Critical Reviews™ in Therapeutic Drug Carrier Systems, 2009
In recent years, various nanotechnology platforms in the area of medical biology, including both diagnostics and therapy, have gained remarkable attention. Moreover, research and development of engineered multifunctional nanoparticles as pharmaceutical drug carriers have spurred exponential growth in applications to medicine in the last decade. Design principles of these nanoparticles, including nano-emulsions, dendrimers, nano-gold, liposomes, drug-carrier conjugates, antibodydrug complexes, and magnetic nanoparticles, are primarily based on unique assemblies of synthetic, natural, or biological components, including but not limited to synthetic polymers, metal ions, oils, and lipids as their building blocks. However, the potential success of these particles in the clinic relies on consideration of important parameters such as nanoparticle fabrication strategies, their physical properties, drug loading efficiencies, drug release potential, and, most importantly, minimum toxicity of the carrier itself. Among these, lipid-based nanoparticles bear the advantage of being the least toxic for in vivo applications, and significant progress has been made in the area of DNA/RNA and drug delivery using lipid-based nanoassemblies. In this review, we will primarily focus on the recent advances and updates on lipid-based nanoparticles for their projected applications in drug delivery. We begin with a review of current activities in the field of liposomes (the so-called honorary nanoparticles), and challenging issues of targeting and triggering will be discussed in detail. We will further describe nanoparticles derived from a novel class of amphipathic lipids called bolaamphiphiles with unique lipid assembly features that have been recently examined as drug/DNA delivery vehicles. Finally, an overview of an emerging novel class of particles (based on lipid components other than phospholipids), solid lipid nanoparticles and nanostructured lipid carriers will be presented. We conclude with a few examples of clinically successful formulations of currently available lipid-based nanoparticles.
Solid lipid nanoparticles are at the forefront of the speedily developing field of nanotechnology with numerous potential applications in drug delivery, clinical medicine and research as well as in other diverse sciences. SLN combine advantages of the traditional systems but avoid some of their major disadvantages. Lipid nanoparticles offer the possibility to develop new therapeutics along with applicability for various routes such as oral, topical and parenteral. It acts as colloidal drug carriers for hydrophilic or lipophilic drugs. SLNs unite the advantages of polymeric nanoparticles, fat emulsions and liposomes. The ability to incorporate drugs into nanocarriers offers an innovative prototype in drug delivery that could be used for secondary and tertiary levels of drug targeting.
Lipid Nanoparticles as Carriers for Bioactive Delivery
Frontiers in Chemistry, 2021
Nanotechnology has made a great impact on the pharmaceutical, biotechnology, food, and cosmetics industries. More than 40% of the approved drugs are lipophilic and have poor solubility. This is the major rate-limiting step that influences the release profile and bioavailability of drugs. Several approaches have been reported to administer lipophilic drugs with improved solubility and bioavailability. Nanotechnology plays a crucial role in the targeted delivery of poorly soluble drugs. Nanotechnology-based drug delivery systems can be classified as solid lipid nanoparticulate drug delivery systems, emulsion-based nanodrug delivery systems, vesicular drug delivery systems, etc. Nanotechnology presents a new frontier in research and development to conquer the limitations coupled with the conventional drug delivery systems through the formation of specific functionalized particles. This review presents a bird's eye view on various aspects of lipid nanoparticles as carriers of bioact...
Nanotechnology is rapidly expanding research area, encompassing the development of man-made materials in nanometer size range. Nanoscale drug delivery system using various nanomaterials is emerging technology for the rational delivery of many chemotherapeutic agents. Nanoparticles attracted the scientists across many disciplines to engineer many desired properties that might otherwise be incompatible on a single device. Formulation scientists are facing the challenges such as poor solubility and bioavailability of the newly invented drugs. One of the approaches to face the above challenge is to develop the particulate carrier system. Solid lipid nanoparticle or liposphere or nanosphere system is the most feasible particulate carrier system which is an alternative to nanoemulsions, liposomes and polymeric nanoparticles. This system offers added advantages in comparison to other related particulate drug delivery systems. The present review emphasizes on various basic and applied aspects of solid lipid nanoparticles in novel drug delivery system especially techniques involved in their production, characterization and various applications. It also focuses on the drug loading capacity, drug incorporation and factors affecting drug release from this colloidal system.
Nano
The efficacy and safety are two challenging factors before trusting the lipid-based Nanosystems (LBNs) for diagnostic and therapeutic purposes. The aim of this paper is to evaluate the accessible in-vitro and in-vivo studies on the contribution of major physicochemical factors of LBNs for the effective and safe delivery of drugs and anticancer agents into the target site. These factors included lipid charge, particle size and size distribution, lipid composition and components, surface hydrophilicity and hydrophobicity, and surface coating. Here, reliable databases were searched for full-text, accessible and original articles to conduct this review. We included relevant studies since 1992, which were conducted on the development of LBNs for therapeutic and diagnostic purposes. Many studies have shown that using polyethylene glycol modification reduces the undesirable side effects and controls the efficacy and toxicity for in-vitro and in-vivo delivery of drugs or anticancer agents. ...
Journal of Pharmaceutical Investigation, 2017
Drug release from a polymeric nanocarrier is affected by several factors including the sort of composition (drug, polymer, and excipient), the ratio of composition, physical or chemical interaction between components, and manufacturing methods. Depending on the mechanism of drug release from the vehicles, it can be divided into four categories (diffusion, solvent, chemical interaction, and stimulated release). Recently, lipids have attracted great interest as carriers for water-insoluble drug delivery. Lipidbased drug-delivery systems have received a lot of interest because of their ability to improve solubility and bioavailability of drugs that are poorly soluble in water. The lipid carrier, formulation strategy, and rational drug-delivery system should be selected appropriately for a lipid-based drug-delivery system to be successful. In this review, the general release characteristics and mechanisms of drug from nanocarriers will be discussed.