Preparation, Characterization, and Release Study of Tacrolimus-Loaded Liquid Crystalline Nanoparticles

Abstract

GRAPHICAL ABSTRACTThe use of liquid crystalline nanoparticles is a novel approach in the field of controlled drug delivery. Tacrolimus, being a highly lipophilic drug, is easily incorporated in the hydrophobic core of these nanoparticles, which are prepared using monoolein, distilled water, and varying ratios of poloxamer 407. Characterization, including transmission electron microscopy (TEM) images, particle size, and entrapment efficiency analysis suggested the formation of cubosomes with a particle size ranging from 140 to 155 nm and entrapment level of tacrolimus as high as 99% or above. In vitro release studies, revealed a sustained release of tacrolimus for 2 weeks, with a high stability profile of nanoparticles and incorporated drug during the storage period. Therefore, it suggests the possible use of tacrolimus-loaded formulation for intradermal delivery can be useful in the treatment of locally affecting autoimmune skin disease such as psoriasis.

Photoswitchable Fluorescent Liquid Crystal Nanoparticles and Their Inkjet‐Printed Patterns for Information Encrypting and Anti‐Counterfeiting

“…The spontaneous molecular order and resultant anisotropic properties make liquid crystals (LCs) to develop a wide range of display and nondisplay applications . Among them, the confinement of LC molecules within nanocolloids to create nanomaterials widens the range of LC potential applications to areas such as nanoactuation, cell imaging, controlled release, and photonics . The unique property is that the confinement of LC within small volumes at the micro‐ and nanoscale could retain LC ordered arrangement .…”

Entrapment of curcumin into monoolein-based liquid crystalline nanoparticle dispersion for enhancement of stability and anticancer activity

“…[19][20][21]32 In our earlier studies conducted with hydrophobic drugs, the EE was also close to 100%, indicating nonspecific interactions between the drug molecule and the hydrophobic moiety of MO -notably, hydrophobic binding and a van der Waals interaction.…”

“…Earlier, we reported that hydrophobic drugs were efficiently entrapped into monoolein (MO)-based LCNs and that the release of the drugs was sustained up to several weeks without a burst effect. 19,20 Furthermore, we were able to control the release of the drug by incorporating hydrophilic and hydrophobic additives into the LCN. 21 In this study, we prepared curcumin-loaded LCNs (LCN-R [liquid crystalline nanoparticles prepared with Cremophor RH40 as a solubilizer]) with the aid of drug solubilizers and investigated the effect of the LCN on cellular uptake, anticancer activity, and cell cycle distribution on a human colonic cancer cell line (HCT116).…”

Nanomedicine-based drug targeting for psoriasis: potentials and emerging trends in nanoscale pharmacotherapy

“…The penetration studies of microemulsion compared to an ointment were higher and targeting by microemulsion take shorter time for effective treatment of psoriasis [72]. In another study, tacrolimus-loaded in the hydrophobic core of liquid crystalline nanoparticles containing monoolefin and poloxamer showed higher entrapment efficiency and in vitro drug permeation [73]. In another study, Tacrolimus (FK506)-loaded SLNs (FK506-SLNs) were prepared by a modified emulsification and low-temperature solidification method with entrapment efficiency of 88.74%.…”

“…0.5 % dithranol-loaded lipogel applied on 20 patients, shows markedly high efficacy, low irritation and minimum staining of skin and clothes as compared to conventional cream [47,48] Dithranol Niosomes Better permeation found in laca mice abdominal skin as compared to conventional cream, whereas 3 times less permeation founds as compared to liposomal vesicular carriers [50] Dithranol Aquasomes Aquasomes-based formulation showed 43.508% permeation, sustained release and greater skin retention and more stability [52] cAMP Dyphylline Liposomes gel Unilamellars liposome converted to gel with the use of carbopol, found highest skin permeation. More targeted action achieved into the skin as compared to Dyphylline solution and liposomal Dyphylline with PEG base [62] Immunophilins/ T-lymphocytes CsA Iontophoresis based lecithin vesicular carriers As compared to microemulsion, lecithin vesicles-based iontophoresis have better potential in site-specific delivery in psoriasis [65] CsA Multi-compartmental liposomes and microemulsified systems Better entrapment efficiency, higher immunosuppression and better compliance achieved [69] Tacrolimus Liquid crystalline nanoparticles Higher solubility, > 99% entrapment efficiency and permeation achieved because of presence of monoolein; moreover, better anti-inflammatory action against psoriasis as compared to tacrolimus dissolved in PG [73] Tacrolimus Microemulsion Tacrolimus-loaded ME shows higher drug skin (20.95 ± 12.03%…”