Abstract
Oral administration is the best way to administer both traditional and novel drugs because it decreases patient non compliance and can also relieve the pain and discomfort associated with parenteral preparations. However, despite many benefits of oral formulations, a number of disadvantages significantly impair bioavailability. By helping with site specific targeting, nanoparticles can stop drugs from breaking down across different physiological barriers. Lipidic systems are regarded as the most evident among all the emerging nano drug carriers. Lipid carriers that are nanostructured are thus created. As these consist of liquid and solid lipid mixes, which make up the safe lipidic colloidal systems. Surfactants are used in system for stabilization. This lipidic formulation offers improved penetration, longer half-life, decreased clearance and greater drug solubility and improves oral bioavailability of various classes of drugs. A type of lipid-based carrier called Nanostructured lipid carrier replaces a certain amount of solid lipid with liquid lipid to get over some of the main drawbacks associated with Solid Lipid Nanoparticles. Research using Nanostructured lipid carriers show that they may be the most advantageous carrier for improving the oral bioavailability of both hydrophilic and lipophilic medications. The article provides a brief overview of the different types, components and fabrication methods of that are employed in formulations, with a primary focus on typical barriers that affect the bioavailability of drugs delivered orally. The article provides advantages with respect to oral bioavailability enhancement are highlighted in this review.
Introduction
Oral administration accounts for around 60% of medication administration in commercially accessible medicines. Approximately 70% of chemicals that are being studied are poorly soluble and 40% of medications that are currently in the market are also poorly soluble. Certain medications exhibit weak solubility, falling into the second class in the BCS classification, whereas others have substantial first pass metabolism effect. Therefore, it’s critical to improve the drug’s solubility and rate of dissolution, as these factors eventually affect the drug’s oral bioavailability.1 Significant efforts have been undertaken in the last 10 years to create dosage forms based on nanotechnology in order to increase the bioavailability of bioactive molecules. Because of its unique benefits, including their highly stable structure, biodegradability, biocompatibility, effective drug loading and sustained release qualities, lipid nanoparticles have drawn more attention than other types of nanoparticles.2 Because of the unique components of lipid nanoparticles; it is widely known to improve drug absorption when taken orally. Lipid nanoparticles can be broadly classified into three types.
- Solid Lipid Nanoparticles (SLN),
- Nanostructured Lipid Carrier (NLC),
- Lipid Drug Conjugates (LDC).
A nano-particulate carrier system called Nanostructured Lipid Carriers (NLCs) is based on oil-in-water nano-emulsions. Emulsifying agents, fat and water are its main constituents. At room temperature, the lipid phase is composed of both liquid (oil) and solid (fat) lipids. Because the drug dissolves in oil and simultaneously encapsulates in solid lipid, the goal of NLC-based formulation is to produce particles with a solid lipid core and integrated oil for increased loading capacity and regulated drug release. NLCs offer a number of advantages, including decreased polymorphic transition, a low crystalline index, enhanced drug loading, encapsulation efficiency, physical stability, enhanced chemical stability, bioavailability and the controlled release of encapsulated components.3
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Table 1: Commonly Used Solid – Lipid, Liquid- Lipid for development of NLC’s.
| Components | Excipients with their melting point | Drugs used | Role of ingredient |
|---|---|---|---|
| Solid-Lipid.11,12 | Steric acid (67-69°C). | Simvastatin Diacerein Carvacrol Testosterone Undecanoate. | For topical administration-controlled release and acidic protection for the medication. |
| Glyceryl monostearate (54-64°C). | Tamoxifen, Silybin, raloxifene, Atorvastatin | Enhancement of orally bioavailability. | |
| Glyceryl Tripalmitate (61-65°C). | Ranolazine | Enhanced entrapment efficiency and sustained released property. |
|
| Precirol ATO 5 (50-60°C). | Lovastatin, Spironolactone, Saquinavir | Improved bioavailability. | |
| Cetyl palmitate (51.9-55.9°C) | Coenzyme Q (10). | Can help in providing your skin with deep moisture. |
|
| Compritol 888 ATO (65-77°C). | Glipizide, Vinpocetin | Viscosity inducing agent | |
| Dynasan 114 (55-58°C). | Domperidone, raloxifene | Used as an adjuvant, seeding agent in solidification. |
|
| Liquid-Lipid.12,13 | Oleic acid (13 to 14°C) | Glipizide, Testosterone, Undecanoate, Ranolazine, Repaglinide | Utilized throughout the nanoparticle's solution phase production. It regulates the nanoparticles' size and shape. |
| Squalene (-4.8ºC) | Lovastatin | It keeps skin hydrated and protects its moisture barrier. |
|
| Labrafac_CC (<-5, 0ºC) | Clotrimazole | Used as emollient. | |
| Miglyol 812 (6ºC). | Spironolactone, Saquinavir, Vinpocetine. | Having excellent spreadability. | |
| Capmul MCM C8 (60-65ºC). | Diacerien | Emollient Demulcent Analgesic, Improved solubility and oral bioavailability |
|
| Labrafil WL 2609 BS | Tamoxifen | ||
| corn oil (-11ºC) | Beta carotene | lubricant |
Table 2: Some Commonly Used Surfactant in NLC’s Formulation.
| Components | Examples |
|---|---|
| Surfactant | Poloxamer 188 |
| Tween 80 | |
| Pluronic F-188 | |
| Myverol 18-04 K | |
| Sodium Dodecyl Sulfate (SDS) |
|
| Sodium Deoxy Cholate (SDC) |
|
| Polyvinyl alcohol | |
| Lecithin | |
| Dynasan 118 | |
| Solutol HS 15 |
Harakal P, Kulkarni N, Gore S, Khade K, Dhole S. Nanostructured Lipid Carrier to Improve Oral Bioavailability. Indian Journal of Pharmaceutical Education and Research [Internet]. 2025 Jul 15;59(3s):s788–801. Available from: http://dx.doi.org/10.5530/ijper.20255950
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