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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
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