After hydrogen and oxygen, carbon is the third most abundant component present in the cosmos with excellent characteristic features of binding to itself and nearly all elements. Since ancient times, carbon-based materials such as graphite, charcoal, and carbon black have been utilized for writing and drawing materials. As these materials possess excellent chemical, mechanical, electrical, and thermal features, they have been readily engineered into carbon-based nanomaterials (CNMs) such as carbon nanotubes, graphene oxide, graphene quantum dots, nanodiamonds, fullerenes, carbon nano-onions, and so forth. These materials are now widely explored in biomedical applications. Thus, the emergence of CNMs has opened up a gateway for the detection, delivery, and treatment of a multitude of diseases. They are being actively researched for applications within tissue engineering, as vaccine vectors, and for the delivery of therapeutics to the immune system. This review focuses on the recent advances in various types of CNMs, their fabrication techniques, and their application in the delivery of therapeutics both in vitro and in vivo. The review also focuses on the toxicity concern of the CNMs and the possible remedies to tackle the toxicity issues. Concluding remarks emphasize all the CNMs discussed in the review over their possible biomedical applications, while the future perspectives section discusses the approaches to bring CNMs into the mainstream of clinical trials and their therapeutic applications.
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 applications of nanostructured lipid carriers (NLCs) in oral drug delivery for various medical conditions, shedding light on their current regulatory status, including FDA-approved options and those in pre/clinical stages. The review also features patented NLC formulations. It provides valuable insights into how NLCs can be harnessed for effective oral drug delivery and outlines recent advancements in optimizing their performance to tackle gastrointestinal barriers, thus opening new possibilities for NLCs in future pharmaceutical applications.
30 August 2024 in Journal of Drug Delivery Science and Technology
Designing a potential polymer-based drug delivery carrier is of great significance for enhancing the anticancer effectiveness and oral delivery of hydrophobic phytodrugs. Chrysin (CRY) is a potential anticancer phytomolecule; however, its utilization for further applications is restricted due to its low aqueous solubility and poor bioavailability. Here, a biocompatible polymer, i.e. Pluronic F68 modified with stearic acid (F68–SA) was used for the fabrication of chrysin-loaded nanomicelles (CNMs). The fabricated CNMs comprised particles of 142.7 nm size with a spherical shape, amorphous nature, and a drug encapsulation efficiency of 37.06%. The incorporation of a hydrophobic segment into Pluronic F68 significantly enhanced the sustained drug release profile and stability. The CNMs effectively enhanced the anticancer effect against human lung A549 cancer cells, as confirmed by MTT, AO/EB, and cellular uptake assays. Moreover, the fabricated CNMs demonstrated a higher plasma chrysin concentration–time (Cmax) profile compared to a chrysin suspension. The AUC0–t of the CNMs was also 5.6 times higher than that of the CRY suspension. These results indicate that the bioavailability of chrysin was significantly improved due to faster and enhanced absorption after administration as a nanomicelle formulation.
Glaucoma is a neurodegenerative ocular disease characterized by an elevated intraocular pressure (IOP) resulting from impaired aqueous humor outflow, leading to optic nerve damage and potential vision loss. Acetazolamide (ACZ), a carbonic anhydrase inhibitor, is a clinically established diuretic in glaucoma management. The Biopharmaceutics Classification System (BCS) categorizes drugs by their aqueous solubility and intestinal permeability. ACZ, a BCS Class IV drug, exhibits both poor solubility and poor permeability, typically resulting in low oral bioavailability. This investigation focused on developing an ACZ‐loaded nanoemulsion (ACZ‐NE) utilizing biodegradable oily polymer poly(δ‐decalactone) (PDL) to enhance the drug’s solubility, permeability, and therapeutic efficacy. The formulation was optimized via Box–Behnken design and prepared using the nanoprecipitation method. The resultant nanoemulsions (NEs) exhibited favorable ophthalmic characteristics, including a mean droplet size of 238.5 nm, with a narrow polydispersity index, i.e., 0.107, and negative zeta potential (‐−11.9 mV). In vitro release studies demonstrated sustained drug release for up to 14 h, prolonging the therapeutic impact and reducing the need for frequent administration. Ex vivo corneal permeation was significantly enhanced in ACZ‐NE compared to an aqueous drug suspension, indicating enhanced transcorneal permeation ability of NE. In addition, the NE demonstrated ocular safety in the Draize test and effectively reduced IOP for up to 12 h in experimental rabbits. In vivo pharmacokinetic evaluation from the ocular route revealed a prolonged half‐life (1.92 h), increased Cmax (0.083 μg/mL), and AUC 0 −∞ (1360.32 μg·h/mL) relative to the marketed formulation. Histopathological examination confirmed improved ocular tissue integrity following treatment with the developed NE. These findings collectively suggest that the PDL‐based ACZ‐NE not only offers a promising strategy for sustained ocular drug delivery but also has the potential to mitigate the systemic adverse effects associated with conventional oral therapy of ACZ tablets, thereby instilling confidence in its potential to improve patient outcomes.
1. Before the prehistoric period, plants played an important and primary role in human wellness (Cordell 2011). Pharmaceutical companies typically focus on developing synthetic drugs to treat vario...