Background: Acne vulgaris is a common chronic skin disease that affects around 9.4% (approx. 650 million people) of the global population. Growing research in the field of nanomedicine over the years has now been exploited in management of various human disorders. The nanomedicine concept has an immense opportunity for the effective management and control of acne disease by designing a novel, low-dose topical delivery system. Topical nanoemulsion-based gel preparations are said to have various benefits over the conventional formulations. The recent patents on topical anti-acne formulation (US 7241456B2; US 6897238B2; US 6284234B1) provided the concept to design thymol loaded nano-emulgel for topical application in acne. Methods: The objective of the current investigation was to design a thymol loaded nanoemulgel preparation by exploiting low-energy emulsification method for topical application in acne. Furthermore, developed formulation was characterized for thermodynamic stability, mean droplet size, zeta potential, drug content and in-vitro drug diffusion study. Results: The optimized thymol loaded nanoemulsion was found to be 13.60±0.117 nm with PdI 0.197±0.008. Nanoemulsions will provide an enormous surface area for better penetration of therapeutic agent into the pilosebaceous region, resulting better efficacy. Conclusion: From the above studies, it concluded that aqueous-based gel vehicle of the developed formulation system exploited for topical delivery has moisturising properties which can improve local tolerability also.
1 October 2011 in Colloids and Surfaces B: Biointerfaces
The purpose of this study was to formulate carbopol hydrogels containing eugenol-loaded solid lipid nanoparticles (EG-SLNs) for epidermal targeting to treat fungal infections in skin. EG-SLNs were incorporated into carbopol hydrogels and the physiochemical characteristics of EG-SLN in hydrogels were investigated by dynamic light scattering, transmission electron microscopy and atomic force microscopy. Rheological behavior and mechanical properties of hydrogels were also studied before and after incorporation of EG-SLNs. The epidermal-targeting ability of EG-SLN-enriched hydrogels was evaluated by estimation of eugenol in the epidermis of human cadaver skin. An occlusion (hydration) study was also performed to elucidate the mechanism of epidermal targeting of EG-SLN-enriched hydrogels. The particle size (d90) and morphology of EG-SLNs were not significantly changed after incorporation into the hydrogel. EG-SLN of stearic acid-enriched hydrogels follow the Carreau model that describes pseudoplastic flow. The hydrogel containing EG-SLN of stearic acid and of Compritol(®) (Gattefose, Mumbai, India) showed significantly greater accumulation of eugenol in the epidermis (62.65 ± 4.35 and 52.86 ± 3.76 µg/cm(2), respectively) than that of eugenol-hydroxypropyl-β-cyclodextrin complex in hydrogel (9.77 ± 1.16 µg/cm(2)) and almond oil solution of eugenol (3.45 ± 0.6 µg/cm(2)). The occlusion study demonstrated greater hydration of human cadaver skin treated with EG-SLN-enriched hydrogel compared with that of hydrogel and intact skin. Hydrogels containing EG-SLNs could be a promising formulation for epidermal targeting to treat fungal infections in skin.
: Chrysin (a flavonoid) has shown various promising pharmacological activities viz. anticancer, anti-diabetic, immune-modulation, antidepressant, and anti-asthmatic. Additionally, it exhibited potential protective effects against various toxins on different organs like the liver, brain, kidney, and heart. A multitude of studies have been conducted to explore the possible targets for its possible mechanism of action. However, its therapeutic applications have been limited due to its poor oral bioavailability. The major reason for its poor bioavailability is its extensive first-pass metabolism. A critical review of the pharmacological properties of chrysin and its associated molecular targets has not been discussed as yet comprehensively. Therefore, the emphasis of the present work is to provide an in-depth understanding of molecular targets accountable for the pharmacological actions of chrysin. Moreover, a schematic diagram was made for the first time to represent the comprehensive pharmacokinetic properties of chrysin, which helps to understand the biopharmaceutical aspect for its successful delivery. An in-depth understanding of the biopharmaceutical properties of chrysin will help in adopting a suitable formulation approach to overcome poor oral bioavailability. Additionally, it facilitates to study the possible pharmacokinetic interactions of chrysin with other drugs. Hence, we found that chrysin is a miraculous natural agent with myriad therapeutic properties, and its benefit can be exploited with an in-depth understanding of molecular targets, pharmacological actions, and biopharmaceutical attributes.
Glaucoma is a degenerative, chronic ocular disease that causes irreversible vision loss. The major symptom of glaucoma is high intraocular pressure, which happens when the flow of aqueous humor between the front and back of the eye is blocked. Glaucoma therapy is challenging because of the low bioavailability of drugs from conventional ocular drug delivery systems such as eye drops, ointments, and gels. The low bioavailability of antiglaucoma agents could be due to the precorneal and corneal barriers as well as the low biopharmaceutical attributes of the drugs. These limitations can be overcome by employing nanoparticulate drug delivery systems. Over the last decade, there has been a lot of interest in chitosan-based nanoparticulate systems to overcome the limitations (such as poor residence time, low corneal permeability, etc.) associated with conventional ocular pharmaceutical products. Therefore, the main aim of the present manuscript is to review the recent research work involving the chitosan-based nanoparticulate system to treat glaucoma. It discusses the significance of the chitosan-based nanoparticulate system, which provides mucoadhesion to improve the residence time of drugs and their ocular bioavailability. Furthermore, different types of chitosan-based nanoparticulate systems are also discussed, namely nanoparticles of chitosan core only, nanoparticles coated with chitosan, and hybrid nanoparticles of chitosan. The manuscript also provides a critical analysis of contemporary research related to the impact of this chitosan-based nanomedicine on the corneal permeability, ocular bioavailability, and therapeutic performance of loaded antiglaucoma agents.