Flexible liposomal gel dual-loaded with all-trans retinoic acid and betamethasone for enhanced therapeutic efficiency of psoriasis

Abstract

Background Psoriasis is a chronic immune-mediated inflammatory skin disease without effective treatment. The utilization of all trans-retinoic acid (TRA) and betamethasone (BT) for the treatment of psoriasis is still facing difficulties, due to their relatively poor stability, limited skin permeation, and systemic side effects. Flexible liposomes are excellent in deeper skin permeation and reducing the side effects of drugs, which is promising for effective treatment of skin disorders. This work aimed to establish dual-loaded flexible liposomal gel for enhanced therapeutic efficiency of psoriasis based on TRA and BT. Results Flexible liposomes co-loaded with TRA and BT were successfully prepared in our study. The characterization examination revealed that flexible liposomes featured nano-sized particles (around 70 nm), high drug encapsulation efficiency (> 98%) and sustained drug release behaviors. Flexible liposomes remarkably increased the drug skin permeation and retention as compared with free drugs. Results on HaCaT cells suggested that flexible liposomes were nontoxic, and its cellular uptake has a time-dependent manner. In vivo studies suggested the topical application of TRA and BT dual-loaded liposomal gel had the best ability to reduce the thickness of epidermal and the level of cytokines (TNF-α and IL-6), largely alleviating the symptoms of psoriasis. Conclusions Flexible liposomal gel dual-loaded with TRA and BT exerted a synergistic effect, which is a promising topical therapeutic for the treatment of psoriasis.

Interfacial Effects and the Nano-Scale Disruption in Adsorbed-Layer of Acrylate Polymer-Tween 80 Fabricated Steroid-Bearing Emulsions: A Rheological Study of Supramolecular Materials

“…Given the nature of the carbopol molecular skeleton and voluminous polar Tween 80 headgroup, electrostatic or hydrogen-bond like interaction based on the development of partial charges between polymer and surfactant is highly likely [ 5 , 13 , 19 , 22 ]. Similarly, interaction of the polar regions of a drug such as ‘betamethasone class’ and hydrophilic polymer or Tween 80 surfactant either in the monomeric form or encapsulated by virtue of its apolarity, within micellar forms, is also highly likely [ 13 , 14 ] and this is yet further reinforced, as was previously reported for entrainment of hydrophobic entities and molecules (log p > 1.5) in bilayered vesicular carriers [ 15 , 25 ], as might be expected for BMP with a log p value of 1.8.…”

“…Control emulsions were based on Tween 80, as the primary emulsifier with the inclusion of the steroidal drug, betamethasone-21-phosphate (BMP) at a concentration of 0.65 mM, as an interfacial intercalation species, thought to be able to interdigitate with surfactant alkyl chains and polar head groups [ 25 , 26 , 27 ]. Intramolecular interaction between the primary adsorbed layer materials and sublayer materials was indicated previously by both neutron reflectometry [ 34 ] and EPR spectroscopy [ 2 ], used to further investigate the role of carbopols in surface adsorption behavior.…”

“…The steroid (cortico-steroid) class of molecules includes well-known anti-inflammatory therapeutics, such as hydrocortisone, prednisolone, betamethasone [ 25 ] and dexamethasone in addition to sex hormones, such as progesterone and testosterone. All are based on a cholestane tetracyclic triterpene structure with generic skeleton structure of 27 carbon atoms with obvious chemical similarity to their biological precursor, cholesterol.…”

Recent Advances in Liposomal-Based Anti-Inflammatory Therapy

“…In the most prominent anti-inflammatory disease targeted by liposomal drug development, rheumatoid arthritis, innovation is mostly focused on combining several therapies [ 89 , 90 ]. In the other anti-inflammatory disease applications discussed in the current review, such as psoriasis, liposomal formulations are now also considered for combination therapy [ 133 ]. This type of knowledge transfer is essential for the development of novel therapeutic options in all fields of application.…”

Enhancement and Extended Release of the Anti-hypertensive Drug Carvedilol using Optimized Ethosomal Gel via Transdermal Route

“…1 successful entrapment of carvedilol loaded ethosomes in hydrogel for transdermal delivery was possible and the anti-hypertensive effect of the drug was tested on Wister Rats by tail-cuff method. Liposomes in the form of gel have been used to deliver drugs transdermally for psoriasis treatment (11). Hence, in this study hydrogels were tried and tested to ensure better stability and deposition of the intended drug on the skin (12).…”