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Tumor Discovery A comprehensive review of bexarotene
were not mediated through immune activation or overall of CTCL. These soft capsules consist of bexarotene,
lipid biosynthesis. Instead, activation of RXR pathways, PEG400, polyoxyethylene sorbitan monooleate,
neuregulin signaling, and netrin signaling may play a role povidone K 30 BP/USP, and butylated hydroxyanisole.
in restoring myelin integrity and improving cognitive and These ingredients are formulated into a suspension
sensorimotor function. These findings provide insights into and then pressed into soft capsules. The resulting
the mechanisms of chemotherapy-induced neurological capsules exhibit high dispersibility, leading to improved
impairments and offer a potential therapeutic approach to bioavailability compared to oral tablets. Furthermore,
alleviate these effects . these soft capsules effectively conceal the organoleptic
[65]
properties of the drug and significantly enhance its safety
8.4. Proliferation inhibition mechanisms and efficacy [68] .
The study reveals that bexarotene, acting as a PPARγ
agonist, exhibits concentration and treatment duration- 9.1.3. Topical pharmaceutical compositions
dependent anti-tumoral effects in C6 glioma cells. These comprising bexarotene and a corticosteroid (2013)
effects are attributed to the upregulation of PPARγ Assigned to: “Almirall SA” EP2612665A1
levels and subsequent inhibition of NF-κB, resulting in The patent describes topical formulations
DNA damage and apoptosis. Moreover, treatment with comprising bexarotene and a corticosteroid (e.g.,
bexarotene leads to increased oxidant levels and decreased hydrocortisone, clobetasol, betamethasone, prednicarbate,
antioxidant levels in the cells. It is important to note that methylprednisolone, prednisolone, fluocortolone, and
this study solely relies on in vitro experiments and lacks dexamethasone) in combination with a vehicle. The
in vivo validation. Nonetheless, the findings suggest that use of both drugs together showed a synergistic anti-
bexarotene holds potential as a therapeutic agent for psoriatic effect. In addition, the invention discloses a
neuroblastomas .
[66]
method of treating skin diseases using the aforementioned
[69]
9. Review of patents combination of bexarotene and a corticosteroid .
Due to the potential of bexarotene in the treatment of 9.1.4. A kind of bexarotene nanosuspension (2015)
multiple disorders, several patents and patent applications Assigned to: “Liaoning University” CN104922062B
have been filed, with a primary focus on overcoming
typical limitations. A comprehensive list of essential The disclosure pertains to a method of preparing
patents related to bexarotene is provided in Table 3. nanosuspension containing bexarotene and a surfactant,
specifically polyvinylpyrrolidone, in the ratio of 1:1–1:4.
9.1. Patents related to formulations The resulting nanosuspension tends to diminish the toxic
9.1.1. Bexarotene gel and its preparation method effects and improves the bioavailability of this lipophilic
(2004) drug, attributed to the small grain diameter ranging
between 100 and 1000 nm and increased drug levels in the
Assigned to: “Tianjin Pharmaceutical Research Institute” blood. The prepared nanosuspension can be administered
CN100434068C through various routes such as oral, intravenous,
The patent discloses the formula of bexarotene gel ophthalmic, and inhalation .
[70]
that can be directly applied to skin lesions. The main
constituents of this gel were bexarotene, carbonyl ethylene 9.1.5. Bexarotene soft gel capsule and preparation
polymer, organic amine, glycerol, rudimentary alcohol, method thereof (2017)
and water. The application of the gel lowered the drug Assigned to: “Humanwell Puracap Pharmaceuticals
concentration in the blood, significantly mitigating (Wuhan) Co Ltd” US20190038566A1
systemic toxic effects. The study concluded that bexarotene The invention includes the fabrication of bexarotene
gel was a safe, effective, and stable formulation in the soft gel capsules comprising bexarotene, polysorbate, low-
treatment of CTCL . molecular-weight polyethylene glycol, and high-molecular-
[67]
9.1.2. Bexarotene soft capsules and preparation weight polyethylene glycol. The primary objective of this
method thereof (2011) invention is to overcome the problem of drug degradation
caused by high-temperature heat release and degassing
Assigned to: “Tianjin Pharmaceutical Research Institute” during the preparation of the bexarotene soft gel capsules.
CN103181912A The method of preparation involves two steps. First, all the
The invention discloses the method for preparing ingredients are heated and mixed to obtain a mixed melt,
bexarotene soft capsules for the effective management which is then cooled. Second, the cooled mixed melt is
Volume 2 Issue 2 (2023) 10 https://doi.org/10.36922/td.0436

