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Writer's pictureAditya Kaipa

Pharmacokinetics of Curcumin and Nanoformulations

(Now that we understand the classical and non-classical modes of curcumin nucleation and growth, let's take a look at how curcumin is employed and studied in pharmaceuticals)


In the recent decades, several new developments have been adapted to overcome challenges associated with Curcumin-nanomedicines and to augment their anticancer efficacy against specific and broader cancer diseases. Among these developments, the functionalization of Cur-nanomedicines has gained remarkable recognition.



Different formulation strategies have been used to extend the duration of curcumin's retention, bioavailability, improved effectiveness, and regio-specificity in the body. Many dynamic functionalization strategies have been adapted in the design of Cur-nanomedicines including the PEGylation, conjugation of targeting ligand(s), pH-responsiveness, co-delivery of multiple therapeutics, and multi-functionalization.


(A brief overview of the effects of a select few curcumin-loaded nanoformulations on different cancer diseases (Source))


For instance, curcumin nanoparticles (curc-np), which inhibited in vitro growth of drug-resistant bacteria growth and enhanced wound healing in an in vivo mouse wound model. Curc-np may represent a novel topical antimicrobial and wound healing adjuvant for infected burn wounds and other cutaneous injuries (Friedman et. al., 2015). Curcumin-phospholipid complexes can increase curcumin's serum retention in rats (Mythri et al., 2007). According to a different study, micellar formulation considerably increases curcumin's MRT (Ma et al., 2007). Mohanty and Sahoo (2010) discovered recently that encapsulating curcumin in glycerol monooleate lengthens its half-life.


(A schematic representation of wound healing activity of nanocurcumin study (Source))


Moreover, Anand et al. (2007) have shown that delivery systems based on polyester nanoparticles are advantageous for hydrophobic substances and improve the bioavailability of medicines that are poorly soluble in water. Since polyesters, like poly(lactic-co-glycolic acid) (PLGA), have varied degradation kinetics, are biodegradable, biocompatible, and have been approved for pharmaceutical usage by the U.S. Food and Drug Administration, they are typically employed in nano-formulations (Park, 1995). Consequently, recent in vitro research has shown that curcumin-loaded PLGA nanoparticles inhibited the development of cancer cells by increasing cell absorption (Anand et al., 2010).


Following encapsulation with PLGA nanoparticles, curcumin's therapeutic actions on metastatic cancer cells are also enhanced (Yallapu et al., 2010). Drug availability and efficacy will be negatively impacted by restricted drug release from formulation materials, such as polylactic acid (PLGA), which is why it is crucial for the formulation system design to allow for easy drug release (Müller, 1991). Therefore, understanding in vitro drug release is essential for drug administration.


Multiple release stages are seen in drug release from PLGA microspheres, including zero order release, lag phase, and initial burst release (Zolnik and Burgess, 2007). Diffusion of the drug associated with the surface and pores controls the first burst release; polymer degradation in conjunction with diffusion controls the lag phase and zero order release (Faisant et al., 2002). Moreover, low molecular weight PLGA nanoparticles showed diffusion-controlled release, as shown by Zolnik et al. (2006). Diffusion, thus, regulates the continuous release of curcumin from nanoparticles made with low molecular weight PLGA. One crucial aspect of a delivery system that is intimately linked to therapeutic pharmacokinetics and efficacy is sustained drug release.


 (In vitro release of C-NPs (Source))


First, within the first 12 hours, 59.0 ± 6.7% of the curcumin released from the PLGA nanoparticles was released in a burst. After that, the medication was released gradually over the course of six days, with 59.0 ± 6.7% to 89.7 ± 1.4% of the C-NPs released. The curcumin nanoparticles' sustained release profile matched the Higuchi diffusion equation (r2 = 0.95) (Higuchi, 1963). Curcumin from PLGA nanoparticles shows a biphasic release characteristic that is in line with earlier studies (Shaikh et al., 2009).

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