Improving Topical Skin Delivery of Monocrotaline Via Liposome Gel-based Nanosystems

Abstract

Background: In this study, a liposomal gel based on a pH-gradient method was used to increase the skin-layer retention of monocrotaline (MCT) for topical administration. Methods: Using the Box-Behnken design, different formulations were designed to form liposome suspensions with optimal encapsulation efficiency (EE%) and stability factor (KE). In order to keep MCT in liposomes and accumulate in skin slowly and selectively, MCT liposome suspensions were engineered into gels. Results: A pH-gradient method was used to prepare liposome suspensions. The optimal formulation of liposome suspensions (encapsulation efficiency: 83.10 ± 0.21%) was as follows: MCT 12 mg, soybean phosphatidyl choline (sbPC) 200 mg, cholesterol (CH) 41 mg, vitamin E (VE) 5 mg, and citric acid buffer solution (CBS) 4.0 10 mL (pH 7.0). The final formulation of liposomal gels consisted of 32 mL liposome suspensions, 4.76 mL deionized water, 0.40 g Carbopol-940, 1.6 g glycerol, 0.04 g methylparaben, and a suitable amount of triethanolamine for pH value adjustment. The results of in vitro drug release showed that MCT in liposomal gels could be released in 12 h constantly in physiological saline as a Ritger-Peppas model. Compared with plain MCT in gel form, liposomal MCT in gel had higher skin retention in vitro. Conclusion: In this study, liposomal gels were formed for greater skin retention of MCT. It is potentially beneficial for reducing toxicities of MCT by topical administration with liposomal gel.

Design and characterization of dual‐pronged liposome‐embedded gel for enhanced dermal delivery

“…The drug content was determined by weighing 0.5 g of liposomal gel (equivalent to 10 mg of active substance) in a volumetric flask (100 mL) followed by addition of methanol to the required volume. After 2 h of stirring, the mixture was allowed to stand for 24 h. Samples were filtered and spectrophotometrically analyzed to determine the content of NSO and VCO (Yu et al, 2019).…”

“…The cell assembly was maintained at 37°C and stirred continuously at 100 rpm using a magnetic stirrer. At predetermined intervals, the receptor medium was removed and immediately replaced with a fresh receptor solution of the same volume for up to 24 h. Drug content was determined spectrophotometrically at 272 and 254 nm for NSO and VCO, respectively (Sudipta et al, 2011; Yu et al, 2019).…”

“…After cleaning the skin, it was homogenized in 20 mL of chloroform: methanol (2:1, vol/vol) mixture. The homogenates were centrifuged at 6000 rpm for 30 min before being filtered (Yu et al, 2019). The drug concentration in the filtrate was determined spectrophotometrically.…”

Berberine Hydrochloride-loaded Liposomes Gel: Preparation, Characterization and Antioxidant Activity

“…Liposomes-gel is a good carrier for transdermal drug delivery, which can reduce the number of administrations and improve patient compliance. 8 Berberine hydrochloride (BBH) is a kind of quaternary ammonium isoquinoline alkaloid, which is a yellow needleshaped crystal. 9 It is a widely used natural medicine, mainly found in plants such as Berberidaceae, Ranunculaceae Juss, and Menispermaceae Juss.…”

Vitamin E in Atopic Dermatitis: From Preclinical to Clinical Studies

“…Lately, incorporation of micronutrients in nanotechnology-based therapeutics has been shown to improve the bioavailability of poorly aqueous solubility vitamins [20]. Vitamin E nanoformulations have been found to be advantageous in enhancing the delivery efficacy and skin retention [21-23]. In this review, we aim to summarize the current available studies and evidence pertaining to the efficacy and safety for the use of vitamin E treatment in AD, and hence its future prospects.…”