Lipid-Based Nanocarriers: Development and Assessment for Treatment of Hypertension
DOI:
https://doi.org/10.52783/jns.v14.2101Keywords:
Lipid-based nanocarriers, hypertension therapy, sustained drug release, targeted drug deliveryAbstract
Introduction: Worldwide, hypertension continues to be a leading cause of cardiovascular disease-related illness and death. Problems with systemic side effects, inadequate bioavailability, and patient compliance are common with traditional antihypertensive treatments. Nanoemulsions, liposomes, and solid liposome nanocarriers (SLNs) are lipid-based nanocarriers that show promise for improving medication solubility, stability, and targeted administration. Optimizing the formulation parameters and evaluating the pharmacokinetic and pharmacodynamic performance of lipid-based nanocarriers for the efficient delivery of antihypertensive medicines is the goal of this work.
Materials and Methods: A modified method of high-energy emulsification and sonication was used to create nanocarriers based on lipids. Cholesterol, surfactants, and phospholipids served as stabilizers in the mixture. The drug release kinetics, entrapment efficiency, zeta potential, particle size, and formulation of the nanocarriers were studied. Various storage conditions were used to conduct stability experiments. Isolated rat intestinal membranes were used for ex vivo permeability experiments, and a dialysis membrane diffusion method was used for in vitro drug release evaluations. Using non-invasive blood pressure monitoring for four weeks, the in vivo antihypertensive effectiveness was evaluated in Wistar rats. Pharmacokinetic characteristics, such as C_max, T_max, and AUC, were ascertained through the use of LC-MS processing.
Results: The optimized nanocarriers made of lipids showed good colloidal stability, with a zeta potential ranging from -25 to -35 mV and an average particle size of 120-180 nm. Various lipid compositions resulted in entrapment efficiencies ranging from 75% to 90%. A 24-hour sustained drug release profile was shown in in vitro release tests, beginning with a burst effect and progressing through controlled diffusion. Research on the drug's penetration outside of living organisms revealed a 2.5-fold improvement over standard formulations. Oral bioavailability was shown to be significantly improved (an increase in AUC of 1.8-fold), suggesting greater drug absorption, according to pharmacokinetic studies. The antihypertensive efficacy experiments conducted in living organisms showed a notable decrease in both systolic and diastolic blood pressure (p < 0.05), along with longer-lasting therapeutic benefits when contrasted with the free medication.
Conclusion: Nanocarriers based on lipids provide hope for increasing the therapeutic efficacy and bioavailability of antihypertensive medications. An improvement in blood pressure management was achieved with the new formulation due to sustained drug release, better permeability, and improved pharmacokinetics. The results show that lipid-based nanocarriers have promise as a clinical tool for hypertension treatment, which could lead to better patient compliance and less frequent dosing.
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