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Lipids in Drug Delivery
Polymers in Drug Delivery
Lipids are organic molecules that are made up of fatty acids or their derivatives, which are both hydrophobic and hydrophilic. Because they are biocompatible, multifunctional, and can enhance pharmacokinetics, lipids play a key role in the current drug delivery system. Lipids are excellent solubility modifiers that make hydrophobic drugs more soluble and improve the chemical stability of drugs by forming stable nanostructures.
Lipid carriers like liposomes, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs) have been extensively employed to deliver drugs targeted in order to increase therapeutic efficacy and minimize unwanted side effects. Furthermore, the amphiphilic nature of lipids allows them to encapsulate both hydrophilic and hydrophobic drugs, thus realizing diverse drug delivery needs.
Figure 1. Lipid-based drug delivery systems[1].
In recent years, lipids have been instrumental in the delivery of nucleic acids, particularly mRNA vaccines. Lipid nanoparticles (LNPs) enable the protection of mRNA, bringing it to the cells to provoke an immune response. This technology has already been utilised for Covid-19 vaccines, including mRNA-1273 and BNT162b2, which represents a big milestone for lipids in nucleic acid delivery. Second, lipid-based vectors hold great promise for therapeutic siRNA and gene editing technology.
Lipids for drug delivery can be grouped together based on structural and functional properties. In our catalog, we have a wide range of regular liposomes.
Alfa Chemistry has a broad selection of lipid molecules for drug discovery and development to cater to the increasing demand for new ways to deliver drugs. If you are not able to find what you are looking for in our product lineup, contact us. We also offer custom synthesis of novel lipid molecules at high speed and unparalleled formulation development for your advanced pharmaceutical and biotech research.
Liposomes
Liposomes are globular molecules wrapped in a bilayer of lipid-like molecules that can hold both hydrophilic and hydrophobic drugs. They facilitate the entry of drugs into target cells by mimicking the fusion of biological membranes with cells, improving drug bioavailability. The liposome surface can also be tailored with ligands or polymers (e.g., polyethylene glycol, PEG) for targeted targeting and cycling stability. Doxorubicin liposomes (Doxil) have also been used for the treatment of cancer, and they are efficacious in that they can extend the time that the drug circulates in the body and reduce cardiotoxicity.
Solid Lipid Nanoparticles (SLNs)
SLNs are nanocarriers prepared from biocompatible lipids with good drug-loading capacities and physicochemical stability. These nanoparticles are able to control drug release by modulating the lipid composition and protecting the drug from degradation. SLNs have shown, for instance, an anti-inflammatory activity that lasts longer and has fewer side effects in the administration of the anti-inflammatory agent trimethoprim.
Nanostructured lipid carriers (NLCs)
NLCs are new lipid carriers, engineered around SLNs, that enhance drug encapsulation efficiency and drug release properties by injecting liquid lipids into the lipid matrix. Optimisation of this structure makes it easier to use drugs in nonsolvable compounds, like NLCs, which significantly enhance the stability and efficacy of the drug in the delivery of the anticancer agent paclitaxel.
Mature cell permeability and the vulnerability to nuclease degradation are still major hurdles to oligonucleotide therapy. Hence, effective delivery systems are necessary for oligonucleotide conversion to therapeutically useful materials. Neutral lipid-oligonucleotide affixes have become the subject of much attention, reducing the risk of immunogenesis while maintaining in vivo tolerance to high doses.
Alfa Chemistry chemically bonds oligonucleotides to hydrophobic fractions (cholesterol, squalene, fatty acids, etc.) to modify their pharmacokinetic activity and transmembrane delivery. Alfa Chemistry has a dedicated technology platform to provide customers with lipid-affix-based delivery systems for the delivery of siRNA, ASO, and other oligonucleotide therapeutics.
Because of their increased surface area, bulk properties, and better pharmacokinetics, polymers have become a part of drug delivery systems. They do not require as long a circulation time as conventional small-molecule drugs and so can target the tissues in a more targeted fashion. Polymers are used widely in polymer therapeutics and nanomedicines. They are in drug formulations and drug delivery systems.
The main types of polymers commonly used in drug delivery are natural and synthetic:
Figure 2. Overview of polymeric-based drug delivery systems[2].
Nanoparticles made of polymers are excellent carriers for small-molecule drugs, proteins, or nucleic acids. PLGA, for instance, with its products of lactic acid and hydroxyacetic acid as biodegraders, is safe and non-toxic and is FDA-approved for use in a number of formulations. By surface-modifying PEG, the nanoparticles can become long-living and not quickly cleared away by the immune system.
Polymer microspheres enable the slow release of drugs by controlling the rate of polymer degradation. Polymer microspheres, for instance, are injected to provide persistent insulin release for the treatment of diabetes, saving on shots. Polymer microneedles deliver vaccines or small molecules into the skin with minimal incisions and more patient compliance.
There's a 3D network structure in hydrogels that holds lots of water and makes it soft. Polymer hydrogels can be used for local drug delivery and implant long-term stability, and the design (e.g., pH, temperature) makes release very precise.
Polymeric carriers (e.g., polyethyleneimine, PEI) are also very popular as gene carriers because they are extremely compressible to the nucleic acid. Moreover, nucleic acid carriers can be much more stable and effective in terms of delivery when polymers are complexed with lipids or other non-organic molecules.
Polymers extend the life of drugs by packaging them or entangling them and shielding them from environmental damage (i.e., enzymes, pH). PLGA nanoparticles, for instance, harden refractory anticancer drugs and make them more effective.
Polymeric carriers can be surface-engineered with ligands (e.g., antibodies, peptides, or oligonucleotides) for localization in tumour cells or at receptors.
Polymers with their programmable degradation processes can regulate the rate of release of drugs for therapeutic benefit over time. PLGA microspheres, for instance, provide long-term release of drugs for weeks to months.
Polymer nanoparticles - called polymeric nanoparticles (PNPs) - have been widely studied for drug delivery in various antitumor drugs because they can be tuned in terms of their physical-chemical behavior to optimize drug loading and release. Alfa Chemistry is an expert in oligonucleotide therapy delivery technology and provides the technologies to maximize the delivery effectiveness and safety of oligonucleotide therapies.
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