article · Drug Delivery
Orally administered nanoparticles often face reduced absorption because intestinal mucus is continually secreted and shed. To tackle this, a multifunctional chemical conjugate called N-acetyl-L-cysteine-polyethylene glycol (100)-monostearate, or NAPG, was created to coat nanostructured lipid carriers carrying curcumin. The resulting spherical nanoparticles measured between 89 and 141 nanometres, carried a negative charge, and successfully trapped over 90 percent of the drug while providing sustained release. Testing in rat intestinal models showed that increasing the NAPG coating significantly boosted curcumin absorption. Pharmacokinetic tests in rats confirmed that oral bioavailability rose in step with the level of NAPG modification. The formulation with the highest coating amount enhanced curcumin exposure roughly 499-fold compared to a basic curcumin solution and nearly 117-fold compared to uncoated nanocarriers, indicating strong potential for delivering poorly soluble and poorly permeable drugs.
Many therapeutic compounds fail as oral medicines because they cannot easily pass through the intestinal mucus layer into the bloodstream. By engineering nanocarriers that improve both adhesion to and penetration through this protective barrier, pharmaceutical researchers can drastically improve the absorption of hard-to-absorb compounds, potentially turning ineffective oral candidates into viable treatments.
This technology offers an oral drug delivery platform for pharmaceutical developers working with BCS class IV drugs, which suffer from poor solubility and poor permeability. By significantly improving oral absorption, it could support oral reformulations of poorly bioavailable compounds. At present, the research is at an applied preclinical stage, having been synthesised and validated in laboratory settings and live rat models, and would require clinical testing before reaching real-world use.
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The application of orally administered nanoparticles in the circulation system is limited by the secretion and shedding of intestinal tract mucous layer. In order to enhance mucoadhesion and mucus penetration of curcumin (Cur)-loaded nanostructured lipid carrier (NLC) after oral administration, a new multifunctional conjugate, N-acetyl-L-cysteine-polyethylene glycol (100)-monostearate (NAPG), was synthesized. Functionalized nanocarriers (Cur-NAPG-NLC) modified by different amounts of NAPG (the amounts of NAPG were 20, 50, and 100 mg) were prepared and investigated for in vitro and in vivo behavior. Mean particle sizes of 89-141 nm with negative zeta potential (-15 to -11 mV) and high encapsulation efficiency (EE, >90%) possessing spherical and stable nanocarriers were observed. Sustained drug release was also observed for the NAPG-NLC. In situ intestinal perfusion studies showed that with increasing the amount of NAPG increase absorption of Cur. In vivo oral pharmacokinetic evaluation suggested that the bioavailability of Cur in rats was proportional to the degree of functionalization of NLCs with NAPG. AUC<sub>0-t</sub> of Cur-NAPG100-NLC was improved by 499.45 and 116.89 folds as compared to that of Cur solution and unmodified Cur-NLC, respectively. In conclusion, NAPG modified NLC could be a promising drug delivery system for improving oral performance of BCS class IV drugs.
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DOI: 10.1080/10717544.2017.1391890
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