Background
Pilocarpine HCl is a miotic drug that acts as a M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist, causing ciliary muscle contraction that opens up the trabecular meshwork which allows aqueous humour drainage and a resultant reduction in IOP[1]. Pilocarpine HCl is a hydrophilic drug used for managing IOP in the treatment of glaucoma[2]
Pilocarpine HCl encapsulated by liposomes can keep their integrity and physicochemical properties for at least 15 month[3].Pilocarpine HCl specifically inhibits Candida albicans biofilm formation and pathogenicity through interaction with a muscarinic-like receptor[4]. Pilocarpine HCl has acaricidal activity on larvae (LC50=2.6 mg?mL-1) and engorged females (LC50=11.8 mg?mL-1) of R.(B.) microplus[5]
Pilocarpine HCl have apparent functional protective effects in xerostomia models: an increase in the volume of saliva without any change in salivary content. This prophylactic action of pilocarpine HCl may provide a new clinical treatment for irradiation xerostomia in patients with head and neck cancer[6]. Oral activity responses to pilocarpine HCl are enhanced in neonatal 6-OHDA-treated rats[7]
参考文献:
[1]. Jain N, Verma A, et al. Formulation and investigation of pilocarpine hydrochloride niosomal gels for the treatment of glaucoma: intraocular pressure measurement in white albino rabbits. Drug Deliv. 2020;27(1):888-899.
[2]. Owodeha-Ashaka K, Ilomuanya MO, et al. Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery [published correction appears in Prog Biomater. 2021 Oct 5;:]. Prog Biomater. 2021;10(3):207-220.
[3]. Monem AS, Ali FM, et al. Prolonged effect of liposomes encapsulating pilocarpine HCl in normal and glaucomatous rabbits. Int J Pharm. 2000;198(1):29-38.
[4]. Nile C, Falleni M, et al. Repurposing Pilocarpine Hydrochloride for Treatment of Candida albicans Infections. mSphere. 2019;4(1):e00689-18. Published 2019 Jan 23.
[5]. Castro KN, Lima DF, et al. In vitro effects of Pilocarpus microphyllus extracts and pilocarpine hydrochloride on Rhipicephalus (Boophilus) microplus. Rev Bras Parasitol Vet. 2016;25(2):248-253.
[6]. Asari T, Komatsu Y, et al. Prophylactic effects of pilocarpine hydrochloride on xerostomia models induced by X-ray irradiation in rats. Clin Exp Pharmacol Physiol. 2001;28(7):545-550.
[7]. Kostrzewa RM, Neely D. Enhanced pilocarpine-induced oral activity responses in neonatal 6-OHDA treated rats. Pharmacol Biochem Behav. 1993;45(3):737-740.
盐酸毛果芸香碱是一种缩瞳药，作为 M3 型毒蕈碱型乙酰胆碱受体（M3 毒蕈碱受体）激动剂，引起睫状肌收缩，打开小梁网，允许房水排出，从而降低眼压 [1]。盐酸毛果芸香碱是一种亲水性药物，在治疗青光眼时用于控制眼压[2]
脂质体包封的盐酸毛果芸香碱可保持其完整性和理化性质至少 15 个月[3]。盐酸毛果芸香碱通过与毒蕈碱样受体相互作用特异性抑制白色念珠菌生物膜形成和致病性[4]。盐酸毛果芸香碱对幼虫(LC50=2.6 mg?mL-1)和饱食雌虫(LC50=11.8 mg?mL)具有杀螨活性-1) 的 R.(B.) microplus[5]
盐酸毛果芸香碱对口干症模型具有明显的功能性保护作用:唾液量增加而唾液含量没有任何变化。盐酸毛果芸香碱的这一预防作用可能为头颈癌患者的辐照口干症提供一种新的临床治疗方法[6]。新生 6-OHDA 处理的大鼠对盐酸毛果芸香碱的口腔活动反应增强[7]
Protocol
| Cell experiment [1]: |
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Cell lines
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C.albicans SC5314
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Preparation Method
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Standardized C. albicans SC5314 (1×106 cells/ml) were inoculated in RPMI with or without Pilocarpine HCl on Thermanox coverslips (13mm) within a 24-well tissue culture plate and then incubated for 24h at 37℃.
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Reaction Conditions
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0-50mM
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Applications
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Light microscopy revealed that Pilocarpine HCl inhibited filamentation and biofilm formation in a dose-dependent manner. Furthermore, visually, in the presence of increasing concentrations of Pilocarpine HCl, more C.albicans cells maintained a yeast morphology, suggesting that Pilocarpine HCl was inhibiting the yeast-to-hypha transition. Scanning electron microscopy analysis further confirmed the fact that Pilocarpine HCl inhibited biofilm formation due to inhibition of the yeast-to-hypha transition in a dose-dependent manner.
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| Animal experiment [2]: |
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Animal models
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Male Sprague-Dawley rats, seven-week-old
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Preparation Method
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Each rat was fasted overnight before the experiment, but had free access to drinking water. The rat was anaesthetized with urethane (1.25 g/kg, s.c.) and its body temperature was maintained at 37℃ during the subsequent experiment. After intubating the trachea, the duct of the right parotid gland was cannulated for the collection of saliva. Pilocarpine hydrochloride (0.05, 0.1, 0.2 or 0.4mg/kg in 1mL) or distilled water was administered intraduodenally and the saliva was collected for 120min after this administration
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Dosage form
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0.05, 0.1, 0.2 or 0.4mg/kg in 1mL
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Applications
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The mean salivary output for 120min without pilocarpine hydrochloride was 1.58±0.99μL (n=6). Pilocarpine hydrochloride (0.05-0.4mg/kg, intraduodenal) dose-dependently increased salivary output for 120 min in normal rats, the total volumes being 3.02±0.73μL (0.05mg/kg; n=6), 3.91±0.50μL (0.1mg/kg; n=6; P
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参考文献:
[1]. Nile C, Falleni M, et al. Repurposing Pilocarpine Hydrochloride for Treatment of Candida albicans Infections. mSphere. 2019;4(1):e00689-18. Published 2019 Jan 23.
[2]. Asari T, Komatsu Y, et al. Prophylactic effects of pilocarpine hydrochloride on xerostomia models induced by X-ray irradiation in rats. Clin Exp Pharmacol Physiol. 2001;28(7):545-550.
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