辐射聚合制备复合抗癌药缓释制剂的研究

本文报告了甲基丙烯酸β－羟乙酯（ＨＥＭＡ）在室温下进行辐射聚合制备呋喃嘧啶（ＦＴ－２０７）及丝裂霉素Ｃ（ＭＭＣ）混合缓释制剂的研究，结果表明：药物接受１６．２ｋＧｙ照射后其红外和紫外光谱未见明显改变，说明ＦＴ－２０７及ＭＭＣ受１６．２ｋＧｙ以下的辐射对其结构没有影响。ＨＥＭＡ所固化的混合抗癌药体外释放稳定而持久，血药浓度维持在较低水平，小鼠皮下包埋实验显示出明显的治疗效果。     

褪黑素抗自由基作用及其机制

目的研究褪黑素（ＭＥＬ）的抗自由基作用,并探讨其作用机制。方法以丙二醛（ＭＤＡ）为指标,考察ＭＥＬ对四氯化碳（ＣＣｌ４）或氰化钾（ＫＣＮ）处理小鼠肝或脑组织脂质的保护作用;考察ＭＥＬ对环磷酰胺所致小鼠骨髓细胞微核的影响;观察ＭＥＬ清除羟自由基（·ＯＨ）作用,及对醋氨酚处理小鼠肝谷胱甘肽（ＧＳＨ）含量和大鼠红细胞超氧化物歧化酶（ＳＯＤ）、过氧化氢酶（ＣＡＴ）和全血谷胱甘肽过氧化物酶（ＧＳＨ－Ｐｘ）的影响。结果ＭＥＬ（２．０,１０．０ｍｇ·ｋｇ－１,ｉｐ）能显著对抗ＣＣｌ４或ＫＣＮ所致小鼠肝脏或脑组织丙二醛含量的增加。ＭＥＬ（１０．０ｍｇ·ｋｇ－１,ｉｐ）可明显抑制环磷酰胺引起的小鼠骨髓细胞微核增多。ＭＥＬ（０．０７８～５．０ｍｍｏｌ·Ｌ－１）可直接清除·ＯＨ。ＭＥＬ（１．０,１０．０ｍｇ·ｋｇ－１,ｉｐ）可显著对抗醋氨酚（ＡＡＰ）所致小鼠ＧＳＨ的耗竭作用。ＭＥＬ（１．０,５．０ｍｇ·ｋｇ－１,ｉｐ）亦可显著提高大鼠红细胞内ＳＯＤ、ＣＡＴ、全血ＧＳＨ－Ｐｘ活性。结论ＭＥＬ可保护脂质和核酸免受过氧化损伤,这可能与其直接清除·ＯＨ,提高机体ＧＳＨ含量及增强ＳＯＤ、ＣＡＴ、ＧＳＨ－Ｐｘ活力有关。     

白芍总甙对应激大鼠下丘脑一垂体一肾上腺轴和免疫功能的调节

本文以血浆皮质酮（ＣＳ）、促肾上腺皮质激素（ＡＣＴＨ）和β－内啡肽（β－ＥＮＤ）含量为指标，观察了白芍总甙（ＴＧＰ）对不同状态（正常或不同应激）的大鼠下丘脑－垂体－肾上腺轴（ＨＰＡＡ）及其免疫功能的调节作用。结果表明，ＴＧＰ对正常大鼠的ＨＰＡＡ呈现小剂量（１２．５～５０．０ｍｇ·ｋｇ－１）兴奋（血浆ＣＳ含量升高）和大剂量（１００～２００ｍｇ·ｋｇ－１）抑制（血浆ＣＳ含量降低）的剂量依赖性调节作用。其次，ＴＧＰ可兴奋轻度应激（２０℃水游泳）大鼠的ＨＰＡＡ和抑制重度应激（４℃水游泳或２４ｈ束缚）大鼠的ＨＰＡＡ，使过高的血浆ＣＳ、ＡＣＴＨ和β－ＥＮＤ含量降低，提示ＴＧＰ对应激大鼠ＨＰＡＡ呈现轴机能依赖性的调节作用。此外，ＴＧＰ在降低束缚应激大鼠血浆ＣＳ、ＡＣＴＨ和β－ＥＮＤ水平的同时，上调受抑大鼠脾淋巴细胞ＣｏｎＡ增殖反应和腹腔Ｍ释放Ｈ２Ｏ２，提示ＴＧＰ的免疫调节作用可能与其调节ＨＰＡＡ的功能有关。     

绞股蓝总皂苷对NCTC11637株HP延缓大鼠实验性胃溃疡愈合的治疗作用及其机制

目的探讨绞股蓝总皂苷（ｇｙｐｅｎｏｓｉｄｅｓ,ＧＰ）对ＣａｇＡ（＋）,ＶａｃＡ（＋）ＮＣＴＣ１１６３７株幽门螺杆菌（Ｈｅｌｉｃｏｂａｃｔｅｒｐｙ ｌｏｒｉ,ＨＰ）延缓动物实验性胃溃疡愈合的治疗作用及其机制。方法用醋酸诱发大鼠实验性胃溃疡,以溃疡面积、溃疡面积占腺胃部百分比、粘膜组织内白细胞介素 ８（ＩＬ ８）、ＰＧＥ２、ＭＤＡ、ＳＯＤ、·ＯＨ及溃疡愈合时间为指标,观察ｉｇ给予冻干ＮＣＴＣ１１６３７ＨＰ的影响及给予ＨＰ１ｈ后ｉｇＧＰ的治疗作用。结果单给ＨＰ组,溃疡面积加大,愈合延迟,粘膜组织内ＩＬ ８、ＭＤＡ升高,ＳＯＤ活性下降;·ＯＨ生成无明显变化;损伤粘膜组织内ＩＬ ８升高,ＰＧＥ２亦同时升高。ＨＰ＋ＧＰ组溃疡面积、溃疡面积百分率明显减小;粘膜内ＭＤＡ、·ＯＨ生成抑制,ＩＬ ８、ＰＧＥ２平行下降,ＳＯＤ活性提高。结论ＮＣＴＣ１１６３７株ＨＰ可明显延缓醋酸性大鼠胃溃疡的愈合;绞股蓝总皂苷通过抑制炎症反应过程中ＩＬ ８、ＭＤＡ、·ＯＨ生成,并通过提高ＰＧＥ２和ＳＯＤ活性增强胃粘膜保护机制,对感染ＮＣＴＣ１１６３７株ＨＰ大鼠实验性胃溃疡产生显著治疗作用。     

绞股蓝总皂苷对NCTC11637株HP延缓大鼠实验性胃溃疡愈合的治疗作用及其机制

目的探讨绞股蓝总皂苷（ｇｙｐｅｎｏｓｉｄｅｓ,ＧＰ）对ＣａｇＡ（＋）,ＶａｃＡ（＋）ＮＣＴＣ１１６３７株幽门螺杆菌（Ｈｅｌｉｃｏｂａｃｔｅｒｐｙｌｏｒｉ,ＨＰ）延缓动物实验性胃溃疡愈合的治疗作用及其机制。方法用醋酸诱发大鼠实验性胃溃疡,以溃疡面积、溃疡面积占腺胃部百分比、粘膜组织内白细胞介素８（ＩＬ８）、ＰＧＥ２、ＭＤＡ、ＳＯＤ、·ＯＨ及溃疡愈合时间为指标,观察ｉｇ给予冻干ＮＣＴＣ１１６３７ＨＰ的影响及给予ＨＰ１ｈ后ｉｇＧＰ的治疗作用。结果单给ＨＰ组,溃疡面积加大,愈合延迟,粘膜组织内ＩＬ８、ＭＤＡ升高,ＳＯＤ活性下降;·ＯＨ生成无明显变化;损伤粘膜组织内ＩＬ８升高,ＰＧＥ２亦同时升高。ＨＰ＋ＧＰ组溃疡面积、溃疡面积百分率明显减小;粘膜内ＭＤＡ、·ＯＨ生成抑制,ＩＬ８、ＰＧＥ２平行下降,ＳＯＤ活性提高。结论ＮＣＴＣ１１６３７株ＨＰ可明显延缓醋酸性大鼠胃溃疡的愈合;绞股蓝总皂苷通过抑制炎症反应过程中ＩＬ８、ＭＤＡ、·ＯＨ生成,并通过提高ＰＧＥ２和ＳＯＤ活性增强胃粘膜保护机制,对感染ＮＣＴＣ１１６３７株ＨＰ大鼠实验性胃溃疡产生显著治疗作用。     

Menadione reduced doxorubicin resistance in Ehrlich ascites carcinoma cells in vitro

目的：研究维生素Ｋ３（Ｍｅｎ）降低ＥＡＣ／Ｄｏｘ细胞对阿霉素（Ｄｏｘ）的抗药性．方法：测定谷胱甘肽（ＧＳＨ），细胞膜流动性及谷胱甘肽Ｓ转移酶（ＧＳＴ）活性．细胞存活力以甲基四唑蓝法测定．结果：ＥＡＣ／Ｄｏｘ细胞ＧＳＨ，ＧＳＴ及膜流动性均较ＥＡＣ细胞增加（Ｐ＜００１）．Ｄｏｘ对ＥＡＣ／Ｄｏｘ细胞ＩＣ５０为２２３（１５８－２８８）ｍｇ·Ｌ－１．Ｍｅｎ５或１０ｍｇ·Ｌ－１可降低ＥＡＣ／Ｄｏｘ细胞ＧＳＨ（Ｐ＜００１），１ｍｇ·Ｌ－１对ＧＳＨ无影响（Ｐ＞００５），但可降低细胞膜流动性（Ｐ＜００５）．Ｍｅｎ１，５或１０ｍｇ·Ｌ－１可使ＤｏｘＩＣ５０降低到９．６（７８－１１３），６０（２８－９２），或５３（３９－６７）ｍｇ·Ｌ－１（Ｐ＜００１）．结论：Ｍｅｎ在体外降低ＥＡＣ／Ｄｏｘ细胞对Ｄｏｘ抗药性与对ＧＳＨ的耗竭有关．     

110例消化性溃疡幽门螺杆菌感染多方法检测分析

采用酶联免疫吸附试验（ＥＬＩＳＡ）检测幽站螺杆菌菌血清特异性抗体ＩｇＧ、胃镜活检胃粘膜快速尿素酶测定（ＨＰＵＴ）、胃粘膜组织学切片（ＧＩＭＳＡ）染色三咱方法，对１１０例消化性溃疡病人检测幽门螺杆菌（ＨＰ）感染，其检测出总阳性率分别为：ＥＬＩＳＡ法７２．８２％，ＨＰＵＴ７１．８１％，组织毁片ＧＩＭ－ＳＡ染色５６．３０％。经结果分析；ＥＬＩＳＡ法与ＨＰＵＴ间无差异性（Ｐ〉０．０５），ＥＬＩＳＡ与组织切     

β-胡萝卜素对~(60)Co-γ辐射诱发的大鼠T-淋巴细胞次黄嘌呤鸟嘌呤磷酸核糖转移酶位点突变影响

目的：研究β胡萝卜素（βＣａｒ）对电离辐射诱导的突变的影响．方法：Ｔ淋巴细胞克隆检测法测定大鼠Ｔ淋巴细胞次黄嘌呤鸟嘌呤磷酸核糖转移酶（ＨＧＰＲＴ）位点的突变率和硫代巴比妥酸（ＴＢＡ）法测定大鼠血丙二醛（ＭＤＡ）．结果：６０Ｃｏγ３７５Ｇｙ照射大鼠显著提高ＨＧＰＲＴ位点突变频率，ｉｇβＣａｒ１０和２０ｍｇ·ｋｇ－１，突变频率明显降低（Ｐ＜００５），应用βＣａｒ５ｍｇ·ｋｇ－１变化不甚显著，表现一定的剂量依赖性，同时βＣａｒ也明显降低６０Ｃｏγ诱发的大鼠血中ＭＤＡ水平（Ｐ＜００５）．ＭＤＡ下降水平与ＨＧＰＲＴ位点突变频率降低呈明显正相关性（ｒ＝０９９７８，Ｐ＜００５）．结论：βＣａｒ具有抗电离辐射诱导的突变作用，且这一作用与其抗氧化作用有关．     

二氢埃托啡耐受后小鼠脑内cAMP含量的减少及氨基酸含量的增加

目的：探讨二氢埃托啡（ＤＨＥ）耐受的机制．方法：放免法及反相高效液相色谱荧光检测法测定环腺苷一磷酸（ｃＡＭＰ）及谷氨酸（Ｇｌｕ）、门冬氨酸（Ａｓｐ）、谷氨酰氨（Ｇｌｎ）、ＧＡＢＡ的含量．结果：ＤＨＥ反复ｓｃ８ｄ后产生耐受．小鼠去小脑全脑Ｇｌｕ、Ａｓｐ、ＧＡＢＡ的基础含量分别由对照组的１４１±２１、３０±０４、１８±０８升高至耐受组的１７２±２２、４１±０６、３２±１０μｍｏｌ／ｇ组织，Ｇｌｎ的含量无明显改变．下丘脑及纹状体的ｃＡＭＰ基础含量分别由对照组的２７１±３８、１８９±３１降至耐受组的９６±１５、６５±２１ｎｍｏｌ／ｇ组织，大脑皮层ｃＡＭＰ的含量无明显改变．结论：ＤＨＥ耐受与脑内Ｇｌｕ、Ａｓｐ、ＧＡＢＡ基础含量的升高及下丘脑、纹状体内ｃＡＭＰ的基础含量的降低有关．     

甲苯达唑和吡喹酮对小鼠细粒棘球蚴囊壁的葡萄糖磷酸异构酶和甘油醛磷酸脱氢酶的影响(英文)

目的：测定抗包虫药物对细粒棘球蚴囊壁的葡萄糖磷酸异构酶（ＧＰＩ）和甘油醛磷酸脱氢酶（ＧＡＰＤＨ）的影响．方法：感染细粒棘球蚴囊达８－１０个月的小鼠ｉｇ甲苯达唑（Ｍｅｂ）或吡喹酮（Ｐｒａ）治疗，然后剖杀取囊，用生化方法测定ＧＰＩ和ＧＡＰＤＨ活力．结果：感染小鼠用Ｍｅｂ２５－５０ｍｇ·ｋｇ－１·ｄ－１治疗，连续７－１４ｄ，未见对ＧＡＰＤＨ活力有明显影响．若用Ｐｒａ５００ｍｇ·ｋｇ－１·ｄ－１ｉｇ１４ｄ，囊壁的ＧＡＰＤＨ活力被抑制２６５％．至于ＧＰＩ，仅Ｍｅｂ２５ｍｇ·ｋｇ－１·ｄ－１×１４ｄ组的瘪囊示该酶活力被抑制３３２％．结论：ＧＰＩ和ＧＡＰＤＨ不是有效的抗包虫药的主要作用靶．     

ESR detection and dosimetric properties of irradiated naproxen sodium

In the present work, the electron spin resonance (ESR) dosimetric properties of naproxen sodium (NS) was investigated in the dose range of (2.5-25 kGy). Irradiated NS exhibited a very simple ESR spectrum consisting of a broadened antisymmetric single resonance line not saturating up to 2 mW microwave power at room temperature. The sum of two exponential increasing functions associated with two different radicals of different spectroscopic features and relative weights were found best describing experimental dose-response curve. Radiation induced radicals were observed to be very stable at room temperature but the increase in storage temperature increased very appreciably the decay of the contributing radicals. The results of the simulation calculation based on a model of two radicals showed that two carbon dioxide ionic free radicals (*CO(2))(-) of different orientational and environmental features produced by preferential rupture of carboxyl group from the rest of NS molecules in the crystalline matrix, were, likely at the origin of the experimentally observed ESR spectrum. Features such as good time stability of the signal intensity and relatively high radiation yield (G=0.13) were considered providing NS with potential use as dosimetric material in measuring radiation dose in the range of 2.5-25 kGy by ESR technique.     

Effect of gamma radiation on the physicochemical properties of ciprofloxacin in solid state

The aim of this study was to determine the effect of different doses of gamma irradiation on the physicochemical properties of ciprofloxacin (CF) in solid state as a model drug. Powder of CF has been subjected to different irradiation doses: 0, 15, 25, 50 and 100 kGy from Cobalt-60 source in a Gammacell-220 at a rate of 1.15 Gray/s. The effect of radiation has been investigated using DSC, IR, spectrophotometric scanning and X-ray. The impact of irradiation on drug dissolution was also investigated. In addition, the irradiated samples were observed using scanning electron microscope (SEM). All irradiated samples showed chemical stability upon irradiation at the used irradiation doses. The DSC thermogram showed no change in the melting point (266 °C) indicating that the CF identity existed. These findings were also supported by the existence of the ciprofloxacin principal absorption bands in the IR spectra at frequencies 1,616, 1,498 and 2,845 per cm for C = O stretching band of quinolone, C-N stretching band and N-C stretching band. The decrease in the enthalpy by increasing the dose of irradiation attributed the change in crystalline ciprofloxacin to a more amorphous form. The X-ray diffraction patterns of irradiated powder showed a lesser degree of crystallinity as evidenced by fewer peaks of lower intensity compared with the non-irradiated sample. The characteristics of diffraction peaks relevant to crystalline CF virtually disappeared by increasing the dose of radiation from 15 to 100 kGy. This was also clearly demonstrated by SEM photomicrography. The rate of dissolution of CF samples was increased upon irradiation where irradiation at 100 kGy dose showed the fastest dissolution rate while non-irradiated drug samples showed the slowest dissolution rate. It was also observed that CF powder changed in color with color intensity depending on the irradiation dose. Color change is suggested to be due to surface changes in powder samples. This was verified by spectrophotometric scanning of dissolved powder from both irradiated and non-irradiated samples where no trace of any peaks was noticed in the visible range indicating that no radiolytical intermediates responsible for color change were formed during the irradiation. Thus it could be concluded that, although there were important changes in CF powder physical properties upon exposure to different doses of irradiation, the drug was chemically stable.     

The effect of gamma-irradiation on drug release from bioerodible microparticles: a quantitative treatment

The two major objectives of this study were: (i) to monitor the effect of different gamma-irradiation doses (4-33 kGy) on the release kinetics from 5-fluorouracil (5-FU)-loaded poly(D,L-lactide-co-glycolide) (PLGA)-based microparticles, and (ii) to analyze the obtained experimental data with a new mathematical model giving insight into the occurring mass transport phenomena. Drug release was found to depend significantly on the applied gamma-irradiation dose. Interestingly, the obtained release profiles were all biphasic: a rapid initial drug release phase ("burst") was followed by a slower, approximately constant drug release phase. Surprisingly, only the initial rapid drug release was accelerated by gamma-irradiation; the subsequent zero-order phase was almost unaffected. Importantly, the new mathematical model which is based on Fick's second law of diffusion and which considers polymer degradation was applicable to all the investigated systems. In addition, the gamma-irradiation dose could be quantitatively related to the resulting drug release rate. In conclusion, diffusion seems to be the dominating release rate controlling mechanism in all cases, with a significant contribution of the polymer degradation process.     

Investigation of radiosterilization and dosimetric features of sulfacetamide sodium

In the present work, the spectroscopic and kinetic features of the radical species induced in gamma-irradiated sulfacetamide-sodium (SS) was studied at room and at different temperatures in the dose range of 5-50kGy by electron spin resonance (ESR) technique with the aim of investigating the possibility of radiosterilization and dosimetric features of SS. A model consisting of four radical species of different spectroscopic features denoted as I-IV was found to describe best whole experimental data derived throughout the present work. These species were quite stable at room temperature but relatively unstable above room temperature. Heights of the characteristic resonance peaks measured with respect to the base line were considered to monitor microwave, temperature, time dependent and kinetic features of the radical species contributing to ESR spectrum. Collected experimental data were used to characterize the radical species responsible from ESR spectra through simulation calculations. Possible changes in the IR bands of gamma irradiated SS was also investigated by FT-IR technique, but no definite difference was observed between unirradiated and irradiated IR spectra of SS. As in other sulfonamides, radiation yield of solid SS was found to be very low (G 相似文献   

Study of gamma-irradiation effects on chitosan microparticles

Gamma (γ)-irradiation is finding increasing use in the sterilization of pharmaceutical products. However, irradiation also might affect the performance of drug delivery systems. In this study, the influence of γ-irradiation on the characteristics of chitosan microparticles was investigated. The diclofenac sodium was incorporated into chitosan microparticles by spray-drying method. The chitosan microparticles (placebo and drug-loaded) were irradiated at doses of 5, 15, and 25 kGy using a ⁶⁰Co source. Later, the microparticles were characterized by Fourier transform infrared (FTIR) spectroscopy, electron paramagnetic resonance (EPR) spectroscopy, X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and atomic force microscopy. In addition, microparticles also were evaluated for their sizes, drug content, swelling, and drug release behavior. Encapsulation efficiency of irradiated and nonirradiated microparticles was essentially the same. Notably, surface roughness (rms) of placebo microparticles decreased significantly after γ-irradiation when compared with nonirradiated placebo microparticles. FTIR spectroscopy revealed that γ-irradiation of chitosan microparticles induced neither cross-linking nor formation of new group in the chitosan matrix. EPR spectroscopy results showed that the gamma rays induced only one kind of free radical in the chitosan matrix. Size, crystallinity, and thermal properties of the chitosan microparticles did not change much after γ-irradiation. γ-irradiated microparticles, exhibited a slightly higher drug release rate and low swelling capacity than the nonirradiated microparticles.     

辐照对盐酸利多卡因注射液含量的影响考察

目的:建立测定盐酸利多卡因注射液中盐酸利多卡因含量的方法,并考察盐酸利多卡因注射液吸收不同强度的γ射线辐照后含量的变化。方法:采用高效液相色谱法测定含量。色谱柱为Diamonsil-C18,流动相为1%磷酸缓冲液(三乙胺调pH至3.0)-乙腈=80:20,流速为1.0mL.min-1,检测波长为254nm。将同一批号的盐酸利多卡因注射液置于60Co-γ射线放射源中,一次性吸收1、2、4、8、16、25kGy的辐照剂量后检测药物含量。结果:盐酸利多卡因检测浓度线性范围为80～200μg.mL-1(r=0.9998);低、中、高浓度的平均回收率分别为99.55%、99.13%、99.90%;日间及日内RSD(n=3)均小于2%;当吸收辐照剂量在2kGy以上时样品含量变化较大,2、4、8、16、25kGy辐照后含量分别约为152、149、148、138、121μg.mL-1(基础值160μg.mL-1),辐照强度增加与含量下降呈线性关系(r=0.9862)。结论:所建立的高效液相色谱法可用于盐酸利多卡因注射液的含量测定;辐照对盐酸利多卡因注射液的稳定性具有显著影响。     

The effect of ionizing radiation on some derivatives of 1,4-dihydropyridine in the solid state

The effect of gamma and beta radiation in doses between 10 and 100 kGy on physico-chemical properties of four derivatives of 1,4-dihydropyridine (nifedipine, nitrendipine, felodipine and nimodipine) in the solid state was analysed. A number of qualitative and quantitative methods such as UV, IR, TLC, GLC, DSC, EPR as well as organoleptic and gravimetric analysis were used to determine and analyse any changes resulting from irradiation. In order to determine the effectiveness of sterilization with ionizing radiation of doses from 10 to 25 kGy, various microbiological tests were used. It was established that only doses 10-20 kGy of both kinds of radiation ensure total sterilization without any degradation of physico-chemical properties of the compounds studied. For the doses 50-100 kGy a decrease in the content of the compounds, appearance of the products of their decomposition and changes in the melting point and IR spectra appeared. Felodipine (with chlorophenyl substituent) was found to be much more sensitive to ionising radiation than nifedipine, nitrendipine and nimodipine (all with nitrophenyl substituent).     

~(60)Co辐照灭菌对NAO-PLA微球理化特性及体外释放的影响

以 DL-聚乳酸(PLA)为囊材,醋炔诺酮肟(NAO)为主药的微球,可望作为长效避孕注射剂。由于 PLA 的玻璃化温度(T_g)较低,该微球不能采用一般的加热灭菌方法。本文采用10和25kGy 的两种~(60)Co辐照剂量对微球灭菌。对灭菌效果、NAO 和 PLA 以及微球灭菌前后的理化特性和体外释药速率等的比较,表明辐照剂量以10kGy 为宜。     

Preparation and characterization of spray-dried mucoadhesive microspheres of ketorolac for nasal administration

The objective of this investigation was to prepare mucoadhesive microspheres of ketorolac for nasal delivery to avoid gastrointestinal side effects of conventional dosage form. Mucoadhesive microspheres were prepared using carbopol, polycarbophil and chitosan as polymer by spray drying method. The process and formulation parameters were varied to study the effect on the yield and particle size. Microspheres were characterized for surface morphology, encapsulation efficiency, swelling behavior, mucoahesion properties, interaction studies using FTIR and DSC, in vitro drug release, ex vivo nasal cilio toxicity studies and in vivo anti-inflammatory and analgesic activity. Prepared microspheres were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 79-92%. The results showed that the process parameters significantly affect the particle size (10.29-16.75 μm) and yield of microspheres (36.53-56.69%). Interaction studies revealed that there were no drug to polymer interactions. Prepared microspheres exhibited good swelling and mucoadhesion strength which confined the strong mucoadhesive property of microspheres. Ketorolac release from the microspheres was extended up to 8 h and exhibited fickian drug release kinetics with best fit to higuchi model. The drug loaded microspheres were found to be nontoxic to nasal mucosa. The anti-inflammatory and analgesic effects of formulation showed a significant increase (p < 0.05) in percent inhibition value of up to 8 h when compared with ketorolac. In conclusion, spray dried microspheres based on chitosan could be suitable nasal delivery system for the administration of ketorolac.