An accelerated method to evaluate thymopentin release from microspheres in vitro

To design an accelerated method to evaluate thymopentin release from PLGA microspheres in vitro. Microspheres were prepared by double emulsion technique, using poly（lactide-co-glycolide） （PLGA） as carrier. At higher medium temperature （45℃, 50℃ and 55℃）, an accelerated release testing in short time was studied and correlated with the conventional release （37℃） in vitro. The release in vitro of thymopentin from PLGA microspheres at 45 ℃, 50℃ and 55℃ was significantly accelerated （P 〈 0.05）. In particular, at 50℃, an accelerated release （30 h） of the hydrophilic peptide from the PLGA matrix was achieved and correlated well with the conventional release （30 d）. An accelerated release testing in vitro at higher temperature could be used to monitor thymopentin release from PLGA microspheres.

Solid-phase Synthesis of Thymopentin Derivative and Its Immune Regulatory Activity

Thymopentin derivative（septapeptide） was prepared by means of the solid-phase peptide synthesis method in which stepwise and segment condensations were involved. The structures of the key intermediate and target molecule were confirmed by ESI-MS, elementary analysis, IR,^1H NMR and ^13C NMR spectrometries in our experiments. In this study, the authors found that both thymopentin derivetive（septapeptide） and thymopentin could promote T cell proliferation and increase of E-rose fomation cells.

Chemo-enzymatic Synthesis of Z-Asp-Val-Tyr-NH_2——A Precursor Tripeptide of Thymopentin

Z-Asp-Val-Tyr-NH2,a precursor tripeptide of thymopentin（TP-5）,was successfully synthesized by a combination of chemical and enzyme methods.Firstly,the precursor dipeptide Val-Tyr-NH2 was synthesized by a novel chemical method in four steps including the preparation of NCA-Val,the esterification of L-tyrosine and the ammonolysis of L-tyrosine ethyl ester,and the formation of Val-Tyr-NH2 from NCA-Val and L-Tyr-NH2.Secondly,a thermolysin,thermoase PC 10F was used to catalyze the formation of Z-Asp-Val-Tyr-NH2 in an aqueous/organic solvent diphase system with Z-Asp-OH and Val-Ty-NH2 as the substrates under thermodynamic control.The optimum conditions were pH=6.5,40 ℃,thermoase 100 mg,in 2-（N-morpholino） ethanesulfonic acid MES/NaOH（containing 5 mmol/L CaCl2） of n-butanol system（15/85,volume ratio） for 20 h in a maximum yield of 27.02%.

Effects of ulinastatin combined with thymopentin on cellular immunity, humoral immunity and stress response in severe pneumonia

Objective:To explore the effects of ulinastatin combined with thymopentin on cellular immunity, humoral immunity and stress response in severe pneumonia.Methods: A total of 102 cases of severe pneumonia treated in our hospital from February 2016 to November 2017 were collected as subjects and randomly divided into the control group (n=51) and the observation group (n=51), the two groups were treated with routine symptomatic treatment. The control group was treated with the ulinastatin on the basis of routine treatment, the observation group was treated with thymopentin on the basis of the control group. The changes of cellular immunity, humoral immunity, stress response and liver function in the two groups were compared.Results: Before treatment, there was no significant difference in the levels of CD4+, CD8+, CD4+/CD8+, IgA, IgM, IgG, SOD, MDA, T-AOC, AKP, TB and ALT between the two groups (P>0.05). After treatment, the two groups of CD4+ and CD4+ /CD8+ were significantly increased (P<0.05), CD8+ was significantly lower than before treatment (P<0.05), and CD4+ and CD4+ /CD8+ in the observation group were significantly increased compared with the control group (P<0.05), CD8+was significantly lower than the control group (P<0.05);the two groups of IgA, IgM and IgG were significantly increased compared with those before treatment (P<0.05), and the IgA, IgM and IgG in the observation group were significantly higher than those in the control group (P<0.05);two groups of SOD and T-AOC were significantly higher than before treatment (P<0.05), while MDA was significantly lower than before treatment (P<0.05), and SOD and T-AOC in the observation group were significantly increased (P<0.05), and MDA was significantly lower than that of the control group (P<0.05);two groups of AKP, TB and ALT were significantly lower than those before treatment (P<0.05), and the AKP, TB and ALT in the observation group were significantly lower than those in the control group (P<0.05).Conclusions: ulinastatin combined with thymopentin in patients with severe pneumonia can effectively enhance the cellular immunity and humoral immune function, reduce oxidative stress damage and protect the liver function, which has clinical significance.

Effects of lentinan and thymopentin combined with adjuvant chemotherapy on immunity, oxidative stress, matrix metalloproteinases and related factors in patients with tongue squamous cell carcinoma

Objective:To investigate the effects of lentinan and thymopentin combined with adjuvant chemotherapy on immunity, oxidative stress, matrix metalloproteinases and related factors in patients with tongue squamous cell carcinoma.Methods: Retrospective analysis of 78 patients with tongue squamous cell carcinoma admitted to our hospital from February 2013 to November 2017, according to the postoperative chemotherapy scheme, the patients were divided into control group (n=42) and observation group (n=36). The patients in control group were given PF chemotherapy scheme (cisplatin + compound fluorouracil injection), on this basis, the patients in observation group were given lentinan and thymopentin injection combined treatment. The immune index, oxidative stress, matrix metalloproteinase, cyclin D1 (CyclinD1) and B lymphocyte tumor-2 (BCL-2) were detected and analyzed before and after treatment.Results:After treatment, the immunoglobulin level in the control group was not statistically significant compared with that before treatment (P>0.05);the levels of IgA, IgG and IgM in the observation group were significantly higher than those before treatment (P<0.05), and the levels of IgA, IgG and IgM in the observation group were significantly higher than those in the control group (P<0.05);the level of SOD in control group was significantly lower than that before treatment (P<0.05), and the level of MDA was significantly higher than that before treatment (P<0.05);the observation group was the opposite, and its SOD level was significantly higher than that of the control group (P<0.05), and the MDA level was significantly lower than the control group (P<0.05);the levels of MMP-2 and MMP-9 in the two groups were significantly lower than those before treatment (P<0.05), and the levels of MMP-2 and MMP-9 in the observation group were significantly lower than those in the control group (P<0.05);the levels of CyclinD1 and BCL-2 in the two groups were significantly lower than those before treatment (P<0.05), and the levels of CyclinD1 and BCL-2 in the observation group were significantly lower than those in the control group (P<0.05).Conclusions:Lentinan and thymopentin assisted PF chemotherapy regimen can enhance the immune function of patients with tongue squamous cell carcinoma after radical surgery, improve oxidative stress response, inhibit tumor cell proliferation and metastasis. It has the significance of clinical popularization.

The effect on immune function and inflammatory factors of adjuvant antibiotic therapy through Xuebijing combined with thymopentin in elderly patients with severe pneumonian

Objective:To investigate the effect on immune function and inflammatory factors of adjuvant antibiotic therapy through Xuebijing combined with thymopentin in elderly patients with severe pneumonia.Methods:Divided 100 cases of elderly patients with severe pneumonia into the observation group and the treatment group according to odevity of serial number. Fifty patients in each group. Gave control group severe pneumonia conventional treatment, such as mechanical ventilation, antifebrile, removing phlegm and anti-infection, and gave Xuebijing by intravenous drop simultaneously;observation group was given Xuebijing combined with thymopentin by intravenous drop on the base of conventional treatment. Then compared the T lymphocyte subpopulation and serum inflammatory factors level including CRP, IL-6, IL-1 and TNF-α of two groups before treatment and 7 d, 14 d of treatment respectively.Result:(1) There was significant difference in the level of CD3+, CD4+, CD8+, CD4+/CD8+ in this two groups at different time points, and that the level of CD3+, CD4+, CD4+/CD8+: T2>T1>T0, CD8+ level: T2<T1<T0;The increasing range of CD3+, CD4+, CD4+/CD8+level and the decreasing range of CD8+ in the observation group were larger than that in the control group, there was statistical significant difference. (2) The level of serum inflammatory factors CRP, IL-6, IL-1, TNF-α in two groups at different time points were statistical significant difference, all the CRP, IL-6, IL-1 and TNF-α level were T2<T1<T0, presenting a downward trend;The descending range of serum CRP, IL-6, IL-1, TNF-α level in the observation was larger compared with the control group, there was significant difference.Conclusion:The adjuvant antibiotic therapy through Xuebijing combined with thymopentin in elderly patients with severe pneumonia could improve the immune function and lower the inflammatory factors level.

Effect of Xuebijing, thymopentin combined with symptomatic treatment on inflammatory response process in elderly patients with severe pneumonia

Objective:To study the effect of Xuebijing, thymopentin combined with symptomatic treatment on inflammatory response process in elderly patients with severe pneumonia. Methods: A total of 60 elderly patients with severe pneumonia who were treated in the hospital between August 2014 and July 2016 were collected and divided into control group and observation group according to the random number table, 30 cases in each group. Control group received clinical symptomatic treatment, and observation group received Xuebijing, thymopentin combined with symptomatic treatment. The differences in serum pro-inflammatory factors, anti-inflammatory factors as well as liver and kidney function indexes were compared between the two groups before and after treatment.Results: Before treatment, differences in serum levels of pro-inflammatory factors, anti-inflammatory factors as well as liver and kidney function indexes were not statistically significant between the two groups. After treatment, serum IL-1β, IL-6, IL-8, IL-4, IL-13, TB, ALT, AKP, Scr and CysC levels of both groups of patients were lower than those before treatment, and serum IL-1β, IL-6, IL-8, IL-4, IL-13, TB, ALT, AKP, Scr and CysC levels of observation group were lower than those of control group.Conclusion: Xuebijing, thymopentin combined with symptomatic treatment can effectively inhibit the degree of systemic inflammatory response and reduce the liver and kidney function injury in elderly patients with severe pneumonia.

Spectral data analysis and identification of Thymopentin

AIM: To provide a basis for nuclear magnetic resonance (NMR) characterization of polypeptide compounds. METHODS: The 1 H, 13 C NMR and 2D NMR spectra were used to characterize Thymopentin. By using infrared(IR), ultraviolet(UV), mass spectrometry(MS) techniques, along with 1 H-1 H correlation spectrometry (COSY) and distorsionless enhancement by polarization transfer (DEPT), the proton and carbon-13 spectra were assigned completely. RESULTS: The Thymopentin was characterized based on the methods described above. CONCLUSION: The target molecule is confirmed and the structure is identified.

气相色谱法测定胸腺五肽原料药中残留溶剂

目的 采用顶空气相色谱法同时测定胸腺五肽原料药中乙醚、四氢呋喃、甲醇、二氯甲烷、乙醇、乙腈、吡啶和N,N-二甲基甲酰胺等有机溶剂残留量。方法 采用DB-WAX(30 m×0.32 mm×1.00 μm);程序升温:初始温度40 ℃,维持4 min,以10 ℃/min的速率升温至200 ℃,维持3 min;进样口温度为230 ℃;检测器温度为250 ℃;载气为高纯氮气;流速为4 mL/min;分流模式,分流比为10∶1;顶空瓶平衡温度120 ℃;平衡时间为30 min;进样体积为1.0 mL。结果?8种检测残留溶剂在一定浓度范围内显示良好的线性(r>0.997),上述溶剂的定量限分别为1.5、0.1、0.5、0.6、0.8、4.1、0.6、4.4 μg/mL;回收率分别为92.9%、108.4%、106.0%、102.4%、107.5%、109.2%、107.8%和91.2%,RSD值分别为4.1%、2.8%、1.0%、1.9%、1.1%、1.1%、0.6%和1.7%。结论 本法准确、稳定、灵敏度高,可用于胸腺五肽原料药中8种残留溶剂的测定。

胸腺五肽治疗带状疱疹有效性和安全性Meta分析

目的为临床使用胸腺五肽治疗带状疱疹提供证据支持。方法收集中国知网(CNKI)、中国生物医学文献数据库(CBM)、维普(VIP)、万方(WanFang)、PubMed、Embase、The Cochrane Library数据库中有关胸腺五肽治疗带状疱疹的随机对照试验,检索时限为各数据库起自建库至2023年11月。采用Cochrane手册中的RoB 2.0工具对文献进行质量评价,采用RevMan 5.4软件进行Meta分析,并采用GRADE工具评价结局指标的证据等级。结果共纳入文献7篇,均为中文文献,涉及患者471例。Meta分析结果显示,试验组疼痛缓解时间[MD=-1.62,95%CI(-2.29,-0.96),P<0.001],疼痛消退时间[MD=-3.07,95%CI(-3.74,-2.39),P<0.001],有效率[RR=1.13,95%CI(1.04,1.22),P=0.002],不良反应发生率[RR=0.41,95%CI(0.19,0.91),P=0.03]均显著优于对照组,但两组结痂时间无显著差异[MD=-1.12,95%CI(-2.44,0.20),P=0.10]。结局指标的证据等级均为低质量或极低质量。结论胸腺五肽治疗带状疱疹的有效性和安全性均优于单纯抗病毒治疗,但目前结论证据等级均较低,对临床实践缺乏强有力的支撑,需要更多高质量研究证实。

Synergistic immunoreaction of acupuncture-like dissolving microneedles containing thymopentin at acupoints in immune-suppressed rats

Dissolving microneedles carried drug molecules can effectively penetrate the stratum corneum of skin to improve the transdermal drug delivery. The traditional Chinese medicine acupuncture is based on the needle stimulation at a specific location(acupoint) to generate and transmit biochemical and physiological signals which alter the pathophysiological state of patients. However, the pain associated with conventional acupuncture needles and the requirement of highly trained professionals limit the development of acupuncture in non-Asian countries. The purpose of this study is to investigate whether the dissolving microneedles can be utilized as a self-administered painless replacement for acupuncture and locally released drug molecules can achieve expected therapeutic outcomes. Immunosuppressive rats were treated with acupuncture at Zusanli(ST36) acupoint using microneedles containing thymopentin.The immune functions and psychological mood of the immunosuppressed animals were examined. The proliferation of splenocytes was examined by CCK-8 assay. CD4 and CD8 expression patterns in spleen cells were detected by flow cytometry. The current study showed that use of either microneedles containing thymopentin or conventional acupuncture both resulted in immune cell proliferation, which was confirmed by flow cytometry. Furthermore, either conventional acupuncture or microneedles were able to effectively mitigate the anxiety caused by immune-suppression when applied on the ST36.

Implantable sandwich PHBHHx film for burst-free controlled delivery of thymopentin peptide

Sustained release and non-parental formulations of peptides and protein drugs are highly desirable because of enhanced therapeutic effects as well as improved patient compliance. This is especially true for small peptides such as thymopentin(TP5). To this end, implantable sandwich poly(hydroxybutyrate-co-hydroxyhexanoate)(PHBHHx) films were designed to prolong release time and to inhibit burst release phenomenon of TP5 by a simple volatilization method. In vitro release studies revealed that sandwich films had nearly no burst release. In vivo release time of sandwich films was prolonged to 42 days. Pharmacodynamic evaluation demonstrated that TP5 sandwich films significantly increased survival rates in a rat immunosuppressive model and normalized CD4^+/CD8^+ values. These results suggest that TP5 released from sandwich films can attenuate cyclophosphamide's immunosuppressive activity, and possibly achieve results comparable to daily TP5 injection therapy. Thus, sandwich PHBHHx films show excellent potential as a sustained, burst-free release system for small molecular weight, hydrophilic peptide drugs.

部分脾动脉栓塞联合胸腺五肽对乙型肝炎肝硬化脾功能亢进患者细胞免疫和肝纤维化的作用

目的探讨部分脾动脉栓塞术(PSE)联合胸腺五肽对乙型肝炎(乙肝)肝硬化脾功能亢进患者细胞免疫、肝纤维化标记物和肝脏硬度值(LSM)的改善作用。方法选取84例乙肝肝硬化脾功能亢进患者,采用随机数字法分为对照组(n=42)和观察组(n=42)。均行PSE术,术后对照组予以护肝、抗感染、抗病毒及对症支持治疗,观察组在此基础上另予以胸腺五肽肌内注射,疗程24周。6个月后比较两组外周血淋巴细胞亚群(CD^(3+)、CD^(4+)、CD^(8+)、CD^(4+)/CD^(8+))、血清肝纤维化标记物[层粘连蛋白(LN)、Ⅳ型胶原(C-Ⅳ)、透明质酸(HA)、Ⅲ型前胶原(PCⅢ)]水平及LSM(肝脏超声瞬时弹性成像测定)变化。结果6个月后,两组CD^(3+)、CD^(4+)计数百分率和CD^(4+)/CD^(8+)比率较治疗前显著升高(P<0.05),CD^(8+)计数百分率较治疗前显著降低(P<0.05),而观察组CD^(3+)、CD^(4+)计数百分率和CD^(4+)/CD^(8+)比率显著高于对照组(P<0.05),CD8+计数百分率显著低于对照组(P<0.05);两组LN、C-Ⅳ、HA、PCⅢ水平均较治疗前显著降低(P<0.05),而观察组均显著低于对照组(P<0.05);对照组LSM较治疗前无显著降低(P>0.05),观察组LSM显著低于治疗前(P<0.05),且低于对照组(P<0.05)。结论乙肝肝硬化脾功能亢进患者PSE术后使用胸腺五肽可改善细胞免疫功能,降低肝纤维化标记物水平,降低肝脏硬度,综合疗效优于单独PSE,具有较好的临床推广价值。

胸腺五肽对AA肉鸡免疫器官发育的影响

本试验旨在研究胸腺五肽对AA肉鸡免疫器官发育的影响。选用125只14日龄健康AA肉鸡,按体重、性别随机分为5个处理,每个处理25只。从第14天开始,对照组注射生理盐水,4个试验组分别通过胸大肌注射50、150、300、500μg/kg体重的胸腺五肽,1次/d,连续注射5 d。试验分别于用药5 d(19日龄)及停药5 d(24日龄)测定各组肉鸡的胸腺、脾脏和法氏囊的干湿比。结果表明:在19日龄,各处理组间肉鸡脾脏及法氏囊干湿比无显著差异,但50、150μg/kg组肉鸡胸腺g干湿比显著高于300、500μg/kg组及对照组(P<0.05)。在24日龄,各处理组间肉鸡脾脏及法氏囊干湿比仍无显著差异,而50、150μg/kg组肉鸡胸腺干湿比依旧显著高于300、500μg/kg组及对照组(P<0.05)。高剂量胸腺五肽(500μg/kg)并未对肉鸡胸腺、法氏囊、脾脏、肝脏及肾脏造成损伤。综上所述,注射低剂量(50、150μg/kg)胸腺五肽可促进肉鸡胸腺发育,增强机体免疫,且对脾脏和法氏囊无不良影响。

鸦胆子油乳注射液联合胸腺五肽姑息治疗Ⅳ期无驱动基因非小细胞肺癌的效果

目的分析鸦胆子油乳注射液联合胸腺五肽姑息治疗Ⅳ期无驱动基因非小细胞肺癌的效果。方法选取本院2017年4月至2019年11月收治的80例Ⅳ期无驱动基因非小细胞肺癌患者,按照不同的治疗方案将其分为对照组与观察组,各40例。对照组采取胸腺五肽姑息治疗,观察组采取鸦胆子油乳注射液联合胸腺五肽姑息治疗。比较两组的治疗效果。结果观察组的治疗总有效率高于对照组(P<0.05)。治疗后,观察组的最大呼气流量(PEF)、用力肺活量(FVC)及第1秒用力呼气容积(FEV_(1))高于对照组(P<0.05)。治疗后,观察组的白细胞分化抗原3阳性(CD3+)、白细胞分化抗原4阳性(CD4+)高于对照组,白细胞分化抗原8阳性(CD8+)低于对照组,CD4+/CD8+高于对照组(P<0.05)。治疗后,观察组的白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)水平低于对照组,白细胞介素-10(IL-10)水平高于对照组(P<0.05)。治疗后,观察组的癌胚抗原(CEA)、糖类抗原125(CA125)、糖类抗原19-9(CA19-9)水平低于对照组,卡氏功能状态量表(KPS)评分高于对照组(P<0.05)。观察组的生存时间长于对照组(P<0.05)。结论鸦胆子油乳注射液联合胸腺五肽治疗Ⅳ期无驱动基因非小细胞肺癌的效果良好,可改善患者的肺功能、免疫功能,调节炎症因子及肿瘤标志物水平,提升生活质量。

胸腺五肽和人免疫球蛋白辅助治疗AECOPD患者的效果及对外周血Th1、Th2相关细胞因子水平的影响

目的:探讨胸腺五肽和人免疫球蛋白辅助治疗慢性阻塞性肺疾病急性加重期(AECOPD)患者的效果及对外周血Th1、Th2相关细胞因子水平的影响。方法:选取2020年7月—2022年10月在九江市第三人民医院进行治疗的60例AECOPD患者,用信封随机法分成对照组与观察组,各30例。两组均予以常规治疗,对照组予以人免疫球蛋白辅助治疗,观察组基于对照组予以胸腺五肽治疗。观察两组治疗效果,比较两组治疗前后Th1、Th2相关细胞因子、肺功能、免疫功能。结果:观察组治疗总有效率高于对照组,差异有统计学意义(P<0.05);治疗后,观察组白介素-12(IL-12)、γ干扰素(IFN-γ)、CD3^(+)、CD4^(+)水平均高于对照组,白介素-4(IL-4)、白介素-13(IL-13)、CD8^(+)水平均低于对照组,差异均有统计学意义(P<0.05);治疗后观察组改良英国医学研究委员会(mMRC)分级优于对照组,差异有统计学意义(P<0.05)。结论:对AECOPD患者予以胸腺五肽和人免疫球蛋白辅助治疗效果较好,可调节患者Th1、Th2相关细胞因子水平,提高患者肺功能,改善患者免疫状态。

阿奇霉素不同给药方式联合胸腺五肽治疗支原体感染盆腔炎的效果

目的:观察阿奇霉素不同给药方式联合胸腺五肽治疗支原体感染盆腔炎的效果。方法:将125例支原体感染盆腔炎患者随机分为两组,常规组62例,序贯组63例。常规组经口服阿奇霉素联合胸腺五肽注射治疗,序贯组经阿奇霉素序贯给药联合胸腺五肽注射治疗。比较两组炎症因子、子宫血流动力学、不良反应、细菌清除率和病情复发率。结果:治疗后,两组子宫血流动力学无统计学差异(P>0.05),序贯组的炎症因子、不良反应、病情复发率低于常规组,细菌清除率高于常规组,差异均具有统计学意义(P<0.05)。结论:阿奇霉素序贯给药联合胸腺肽治疗支原体感染盆腔炎效果显著。

固相合成胸腺五肽的研究进展

叙述了胸腺五肽TP5的药理、药代及毒副作用、市场状况和前景 ,分析了胸腺五肽各氨基酸的α -氨基保护基和侧链保护基的特点 ,并从固相载体、第一个氨基酸的连接、肽链延长等 3个方面介绍了Merrifield法、Boc法、Fmoc法 。

CD_(14)^+单核细胞人类白细胞抗原-DR预测脓毒症预后及指导免疫调理治疗的初步临床研究

目的 :验证 CD+ 1 4 单核细胞人类白细胞抗原 DR( HL A DR)对于评估严重脓毒症患者免疫功能的作用 ;探讨胸腺 5肽 ( TP 5 )治疗免疫抑制的有效性。方法 :符合严重脓毒症标准 ,CD+ 1 4 单核细胞 HL A DR<30 %的患者被定义为脓毒症免疫抑制和代偿性抗炎症反应综合征 ( CARS)者纳入本研究 ,并接受 1m g TP 5肌肉注射 ,1次 / d,直至 CD+ 1 4 单核细胞 HL A DR>5 0 %或死亡。在 TP 5治疗前及结束治疗时分别测量 CD+ 1 4单核细胞 HL A DR和肿瘤坏死因子α( TNFα)、白介素 6 ( IL 6 )、IL 10和 IL 13。结果 :15例患者存活 ,5例死亡。经 TP 5治疗后所有患者的 CD+ 1 4 单核细胞 HL A DR均有不同程度提高 ,但仅存活者有显著差异。所有患者细胞因子均高于健康对照 ,治疗后存活患者的 TNFα、IL 6明显下降 ;死亡者各种细胞因子变化不明显。结论 :用 CD+ 1 4 单核细胞 HL A DR鉴别脓毒症免疫抑制并指导免疫刺激治疗是安全可靠的 ,且对评估预后有重要价值 ;TP 5可能对逆转免疫抑制有效 ,但需要严格的对照治疗研究确认 ;脓毒症的免疫抑制发生和逆转与促炎 /抗炎细胞因子平衡无关 ,确切机制有待深入探讨。

胸腺五肽pH-敏感壳聚糖纳米粒的制备、体外释放及生物活性

目的为了提高胸腺五肽口服的稳定性及生物利用度,制备胸腺五肽pH-敏感壳聚糖纳米粒并考察其理化性质、体外释放及生物活性。方法采用离子胶凝法制备胸腺五肽壳聚糖纳米粒并用Eudragit S100包衣制备pH-敏感纳米粒;透射电镜和环境扫描电镜观察纳米粒形态;粒度及表面电位分析仪测量纳米粒的粒径及Zeta电位;超速离心法测定载药纳米粒的包封率;动态透析法研究载药纳米粒的体外释放特性;模拟人工消化液考察纳米粒中胸腺五肽的生物稳定性;淋巴细胞增殖反应评价制剂的生物活性。结果pH-敏感胸腺五肽壳聚糖纳米粒的平均粒径为(175.6±17)nm,Zeta电位为(28.44±0.5)mV,包封率为(76.70±2.6)%。胸腺五肽pH-敏感壳聚糖纳米粒具有良好的pH依赖性:在0.1 mol.L-1HCl溶液中累积释放24.65%,在pH5.0 PBS溶液中累积释放41.01%,在pH7.4 PBS溶液中累积释放81.44%。pH敏感壳聚糖纳米粒制剂中的胸腺五肽在人工胃液中稳定,在人工肠液中半衰期为15 min。淋巴细胞体外转化实验表明,胸腺五肽pH-敏感壳聚糖纳米粒保留了TP5的生物活性并且具有浓度依赖性。结论pH-敏感壳聚糖纳米粒可能是口服胸腺五肽的良好载体。