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Innovations and Future Prospects of Dermal Delivery Systems
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
Rashmi Upasani, Anushree Herwadkar, Neha Singh, Ajay K. Banga
Nanostructured lipids are similar to SLN carriers with a difference that they contain a blend of solid and liquid lipids (oils). NLCs have shown to possess a higher drug loading capacity and an improved stability (i.e., reduced drug expulsion) during storage as compared to SLNs. SLNs and NLCs offer several features such as controlled drug release, protection of encapsulated drug from degradation and low skin irritation that make them attractive candidates for dermal application. These nanoparticles also demonstrate occlusive properties thereby helping to maintain skin hydration. Due to their small size, they provide intimate contact with the stratum corneum and thereby have shown to increase permeation for a number of drugs, e.g., clotrimazole, prednicarbate, glucocorticoids, podophyllotoxin and isotretinoin. SLNs and NLCs have also been shown to be effective in targeting drug delivery to certain layers of skin. SLN formulations have demonstrated localized delivery of triptolide in the epidermis, which is the site of action for this drug. The localization further helps to reduce the dosing frequency and hence reducing dose dependent side effects such as irritation. These nanoparticles also act as physical UV blockers and are reported to be an appealing carrier for a number of sunscreen agents.
Development of Ethosome Formulation for Topical Therapeutic Applications
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Mansoureh Nazari Vishkaei, Mohamed B. Khadeer Ahamed, Amin Malik Shah Abdul Majid
A delivery system using micro pellets is another technique which uses the matrix system having a size range of 1–1000 μ. This system can reduce the repeated dosage administration of drugs having less half-life period by releasing the drug in a controlled fashion continuously. In addition, such a system orients the delivery to a targeted site, which can overcome the problem of delivery of two different and incompatible substances at a time and can also exploit for the purpose of taste masking (Zhou et al., 2015). A study reported that the glycyrrhiznic ethosome prepared by the solvent depression method for dermal administration increases skin permeation and significantly enhanced its anti-inflammatory effect (Paolino et al., 2005). The ethosomal formulation of Tripterygium wilfordi (Triptolide) developed using controlled filming rehydration and ultrasonic techniques presented an improved cutaneous permeability, high entrapment, and bioefficiency (Chen et al., 2010).
Why Terpenes Matter—The Entourage Effect
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
Diterpenoid paclitaxel and the semi-synthetic analogue docetaxel have been used in breast and prostate cancers [13,14]. Triptolide is a diterpenoid which has been reported to have antineoplastic activity through inhibiting cell growth at low concentrations and inducing apoptosis at high concentrations [15]. Triterpenoids are close to steroids in structure and are also extensively studied in hormone-related cancers and other types of cancer [16].
Effects of Dietary Phytochemicals on DNA Damage in Cancer Cells
Published in Nutrition and Cancer, 2023
Yang Ye, Ying Ma, Mei Kong, Zhihua Wang, Kang Sun, Fang Li
Triptolide is isolated from Tripterygium wilfordii Hook, a traditional Chinese medicine. Triptolide exerts immunosuppressive, anti-inflammatory, and antitumor effects (142). However, triptolide has been associated with side effects and toxicity in In Vitro and In Vivo experiments (143). Triptolide induces DNA damage and downregulates the expression of genes associated with DNA repair such as ATM, ATR, BRCA-1, and p53 genes to inhibit the proliferation of human malignant melanoma cells (56). Qiao et al. (57) found that triptolide may enhance gemcitabine-induced S phase arrest and DNA double strand breaks by inhibiting checkpoint kinase 1 in pancreatic cancer cells. Moreover, triptolide enhances p53 transcription and activation in laryngeal cancer cells, thereby inhibiting cell proliferation and inducing apoptosis (144). However, triptolide also sensitizes breast cancer cells to doxorubicin before the onset of apoptosis by downregulating ATM expression and inhibiting the DDR (145). Zhang et al. (146) showed that triptolide sensitizes triple negative breast cancer cells (TNBC) to cisplatin by interfering with XRCC1/PARP1-mediated base excision repair and DNA single strand breaks. These studies suggest that triptolide not only improves the sensitivity of cells to chemotherapy drugs, but it also regulates tumor apoptosis through DNA damage mechanisms.
Mechanochemical preparation of triptolide-loaded self-micelle solid dispersion with enhanced oral bioavailability and improved anti-tumor activity
Published in Drug Delivery, 2022
Dabu Zhu, Qiuqin Zhang, Yifang Chen, Minghua Xie, Jianbo Li, Shen Yao, Ming Li, Zhao Lou, Yue Cai, Xuanrong Sun
Triptolide, isolated from a Chinese herb called Tripterygium wilfordii, has been used in Chinese medicine for centuries to treat inflammatory and autoimmune diseases (Gu et al., 2016). In recent years, triptolide has attracted attention for its ability to inhibit growth and accelerate the death of tumor cells in vitro and in vivo (L Liu et al., 2018; Jiang et al., 2019; Tian et al., 2019; Deng et al., 2021). Triptolide exhibits stronger antitumor activity than traditional antineoplastic drugs such as doxorubicin, mitomycin, cisplatin, and paclitaxel (Yang et al., 2003). At present, the marketed triptolide is administrated via oral (tablet dosage forms) and intravenous route (parenteral injections). Despite its curative effects on the various diseases, the clinical application of triptolide has been limited due to its poor aqueous solubility, short half-life in the circulation, and serious side effects.
Transdermal delivery of triptolide–phospholipid complex to treat rheumatoid arthritis
Published in Drug Delivery, 2021
Xin-Yi Liu, Wen-Jun Pei, Ye-Zhen Wu, Fang-Li Ren, Si-Yu Yang, Xiu Wang
In recent years, triptolide has been mainly used for oral and parenteral administration, but it is usually detected in the organs quickly after the administration and excreted via the urinary, fecal, and biliary pathways (Gong et al., 2015; Fan et al. 2018). Due to the high toxicity of triptolide to the kidney, liver, and gastrointestinal tract, the clinical application of triptolide is significantly limited (Tan et al., 2018). There are many advantages of transdermal drug delivery, including avoiding the gastrointestinal irritation of drugs, improving drug stability, maintaining a stable blood concentration, and achieving skin targeted therapy (such as RA). Transdermal drug delivery could deliver triptolide through the skin to the site of arthritis, thus avoiding the toxicity of triptolide. However, triptolide is a highly lipophilic lactone compound with an unstable lactone structure, which is not conducive to percutaneous absorption. Therefore, it is essential to prepare an appropriate formulation to improve the transdermal efficiency and stability of triptolide.