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Vesicular Approach Review on Nanocarriers bearing Curcumin and Applications. 含姜黄素的纳米载体及其应用的囊状方法综述。
Pub Date : 2022-04-04 DOI: 10.2174/2667387816666220404092415
Prashant Upadhyay, Deepak Singh, Sukirti Upadhyay

Phytoconstituents have been used to treat a variety of human diseases for a long time, but their use in pharmaceuticals is limited because of their low aqueous solubility. Researchers have created vesicular systems to address many of the issues associated with the bioavailability and therapeutic efficacy of poorly water-soluble drugs and target the drug to the desired location in the body. Several vesicular nanocarrier systems have been developed. Review contrasts various vesicular drug delivery systems, including liposomes, sphingosomes, emulsomes, niosomes, ethosomes, virosomes, phytosomes, aquasomes, proniosomes, transfersomes, pharmacosomes. Vesicular drug delivery systems have caused a scientific revolution, which has resulted in the development of novel dosage forms. This review aims to illustrate the applications, advantages, and disadvantages of the vesicular approach as nanocarriers bearing curcumin and widely used in gene delivery, tumor-targeting to the brain, oral formulations, and resolving various problems associated with drug stability and permeability issues. Nanocarriers also has wide application as green nanocomposites and for antitubercular drugs depending on their physical properties.

长期以来,植物成分一直被用于治疗各种人类疾病,但由于其水溶性较低,在药物中的应用受到限制。研究人员创建了囊泡系统,以解决与水溶性差的药物的生物利用度和疗效相关的许多问题,并将药物靶向到体内所需的位置。目前已开发出多种囊泡纳米载体系统。综述对比了各种囊泡给药系统,包括脂质体、鞘磷脂体、乳液体、niosomes、ethosomes、virosomes、phytosomes、aquasomes、proniosomes、transferomes、pharmicosomes。囊泡给药系统引发了一场科学革命,导致了新型剂型的开发。本综述旨在说明囊泡方式的应用、优势和劣势,作为纳米载体的姜黄素广泛应用于基因递送、脑肿瘤靶向、口服制剂以及解决与药物稳定性和渗透性相关的各种问题。纳米载体还可作为绿色纳米复合材料广泛应用于抗结核药物,这取决于其物理特性。
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引用次数: 0
Drug delivery platforms containing thermoresponsive polymers and mucoadhesive cellulose derivatives: state of the art and review of patents. 含有热敏聚合物和黏附纤维素衍生物的药物输送平台:技术现状和专利审查。
Pub Date : 2022-04-04 DOI: 10.2174/2667387816666220404123625
J. B. da Silva, R. S. Dos Santos, C. F. Vecchi, M. Bruschi
Nowadays, the development of mucoadhesive systems for drug delivery have gained keen interest, with enormous potential in applications through different routes. Mucoadhesion characterizes an attractive interaction between the pharmaceutical dosage form and the mucosal surface. Many polymers have shown the ability to interact with mucus, increasing the residence time of local and/or systemic administered preparations, such as tablets, patches, semi-solids, micro-and nanoparticles. Cellulose is the most abundant polymer on the earth. It is widely used in the pharmaceutical industry as an inert pharmaceutical ingredient, mainly in its covalently modified forms: methylcellulose, ethylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose and carboxymethylcellulose salts. Aiming to overcome the drawbacks of oral, ocular, nasal, vaginal, and rectal routes, and thereby maintaining patient compliance, innovative polymer blends have gained the interest of the pharmaceutical industry. Combining mucoadhesive and thermoresponsive polymers allows for simultaneous in situ gelation and mucoadhesion, thus enhancing the retention of the system at the site of administration and drug availability. Thermoresponsive polymers have the ability to change physicochemical properties triggered by temperature, which is particularly interesting considering physiological temperature. The present review provides an analysis of the main characteristics and applications of cellulose derivatives as mucoadhesive polymers and their use in blends together with thermoresponsive polymers, aiming platforms for drug delivery. Patents were reviewed, categorized, and discussed focusing the applications and pharmaceutical dosage forms using this innovative strategy. This review manuscript also provides a detailed introduction to the topic and a perspective on further developments.
目前,粘接给药系统的开发已引起人们的极大兴趣,其通过不同途径的应用具有巨大的潜力。黏附的特征是药物剂型与粘膜表面之间的相互作用。许多聚合物已经显示出与黏液相互作用的能力,增加了局部和/或全身给药制剂的停留时间,如片剂、贴片、半固体、微颗粒和纳米颗粒。纤维素是地球上最丰富的聚合物。它作为一种惰性药物成分广泛应用于制药工业,主要以共价改性形式:甲基纤维素、乙基纤维素、羟乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素和羧甲基纤维素盐。为了克服口服、眼、鼻、阴道和直肠途径的缺点,从而保持患者的依从性,创新的聚合物混合物已经引起了制药行业的兴趣。结合黏合剂和热响应性聚合物可以同时进行原位凝胶化和黏附,从而增强系统在给药部位的保留和药物可用性。热响应聚合物具有改变由温度引发的物理化学性质的能力,考虑到生理温度,这一点特别有趣。本文综述了纤维素衍生物作为黏附聚合物的主要特性和应用,以及它们与热敏性聚合物的共混物作为药物传递平台的应用。专利审查,分类,并讨论了重点应用和药物剂型使用这种创新的策略。这篇评论手稿还提供了一个详细的介绍主题和对进一步发展的看法。
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引用次数: 2
Meet the Editorial Board Member 与编辑委员会成员见面
Pub Date : 2022-04-01 DOI: 10.2174/266738781601220408105333
A. Tiwary
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引用次数: 0
Formulation Strategies and Therapeutic Applications of Shikonin and Related Derivatives. 紫草素及其衍生物的处方策略及治疗应用。
Pub Date : 2022-03-02 DOI: 10.2174/2667387816666220302112201
Kirandeep Kaur, Atamjit Singh, Hamayal Sharma, Sanha Punj, Neena Bedi
Shikonin and its derivatives are excellent representatives of biologically active naphthoquinones. A wide range of investigations carried out in the last few decades validated their pharmacological efficacy. Besides having magnificent therapeutic potential, shikonin and its derivatives suffer from various pharmacokinetic, toxicity and stability issues like poor bioavailability, nephrotoxicity, photodegradation, etc. In the recent past, various research groups have developed an extensive range of formulations to tackle these issues to ease their path to clinical practice. The latest formulation approaches have been focused on exploiting the unique features of novel functional excipients which in turn escalate the therapeutic effect of shikonin. Moreover, the codelivery approach in various drug delivery systems has taken into consideration in a recent while to reduce toxicity associated with shikonin and its derivatives. This review sheds light on the essential reports and patents published related to the array of formulations containing shikonin and its derivatives.
紫草素及其衍生物是具有生物活性的萘醌类化合物的优秀代表。在过去的几十年里进行了广泛的研究,证实了它们的药理功效。除了具有巨大的治疗潜力外,紫草素及其衍生物还存在生物利用度差、肾毒性、光降解等药动学、毒性和稳定性问题。在最近的过去,各种研究小组已经开发了广泛的配方来解决这些问题,以缓解他们的临床实践之路。最新的配方方法集中在开发新颖功能赋形剂的独特功能,从而提高紫草素的治疗效果。此外,近年来,各种药物递送系统中的共递送方法已被考虑到减少与紫草素及其衍生物相关的毒性。本文综述了与含有紫草素及其衍生物的一系列制剂相关的重要报告和专利。
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引用次数: 4
Myths and Facts Regarding Particle Size Analysis of Pharmaceutical Powders. 关于药物粉末粒度分析的误区和事实。
Pub Date : 2022-01-01 DOI: 10.2174/2667387816666220704124635
Ravikiran Allada, Hong Heng See
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引用次数: 0
Development of Bromfenac Sodium Loaded Pluronic Nanomicelles: Characterization and Corneal Permeation Study. 溴芬酸钠负载Pluronic纳米胶束的研制:表征及角膜渗透研究。
Pub Date : 2022-01-01 DOI: 10.2174/2667387816666220128123737
Miral Patel, Nithun Saha, Shruti Patel, Priyanka Ahlawat, Abhay Dharamsi, Asha Patel

Background: The Cataract is the leading cause of visual impairment and preventable blindness worldwide. Cataract removal surgery involves various post-operative complications like pain and inflammation.

Objectives: The objective of this study is to screen the polymer concentration as well as optimize the formulation components to develop the pluronic micelles with nanosized characterization and for enhanced corneal permeation study.

Methodology: For optimization, Central Composite design was employed to study the effect of independent variables, concentration of Pluronic F 127 (X1) and the concentration of Hyaluronic acid (X2) on chosen responses (Y 1 ) Micelle size, (Y 2 ) Entrapment Efficiency, (Y 3 ) Viscosity. The lyophilised powder was used for physical characterisation.

Results: The formulation containing 5%w/v Pluronic F127 and 0.2%w/v Hyaluronic acid was the optimised composition with micelle size and zeta potential 38.74±4.12nm and -17.6±0.1 mV respectively. In-vitro drug release was found to be 91.72±1.2 percentage in 8 hours. Surface morphology revealed micelles were spherical in shape. Ocular irritancy study showed that formulation was safe and non-irritant. In vitro corneal permeation studies through excised rabbit cornea indicated 1.5 fold increase in ocular availability without corneal damage compared to an aqueous suspension containing the same amount of drug in nanomicelles.

Conclusion: In a nutshell, Pluronic Nanomicelles would be a platform for the delivery of Bromfenac Sodium.

背景:白内障是世界范围内视力损害和可预防性失明的主要原因。白内障摘除手术涉及各种术后并发症,如疼痛和炎症。目的:本研究的目的是筛选聚合物的浓度和优化配方成分,以开发具有纳米级表征的pluronic胶束,并用于增强角膜渗透的研究。方法:为了优化,采用中心复合设计,研究Pluronic f127浓度(X1)和透明质酸浓度(X2)对选择响应(Y 1)胶束大小、(Y 2)包封效率、(Y 3)粘度的影响。冻干粉末用于物理表征。结果:以5%w/v Pluronic F127和0.2%w/v透明质酸为最优配方,胶束尺寸为38.74±4.12nm, zeta电位为-17.6±0.1 mV。8 h体外释药率为91.72±1.2 %。表面形貌显示胶束呈球形。眼部刺激试验表明,该制剂安全、无刺激性。通过切除的兔角膜进行的体外角膜渗透研究表明,与纳米胶束中含有相同量的药物的水悬浮液相比,在没有角膜损伤的情况下,眼可用性增加了1.5倍。结论:综上所述,Pluronic纳米胶束可作为溴芬酸钠的递送平台。
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引用次数: 1
General Guide to Publish a Scientific Paper. 发表科学论文的一般指南。
Pub Date : 2022-01-01 DOI: 10.2174/2667387816666220429093958
Brahma N Singh, Stefano Giovagnoli
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引用次数: 0
Recent Progress in Hot Melt Extrusion Technology in Pharmaceutical Dosage Form Design. 热熔挤压技术在药物剂型设计中的最新进展。
Pub Date : 2022-01-01 DOI: 10.2174/2667387816666220819124605
Sagar Salave, Kedar Prayag, Dhwani Rana, Prakash Amate, Rupali Pardhe, Ajinkya Jadhav, Anil B Jindal, Derajram Benival

Background: The Hot Melt Extrusion (HME) technique has shown tremendous potential in transforming highly hydrophobic crystalline drug substances into amorphous solids without using solvents. This review explores in detail the general considerations involved in the process of HME, its applications and advances.

Objective: The present review examines the physicochemical properties of polymers pertinent to the HME process. Theoretical approaches for the screening of polymers are highlighted as a part of successful HME processed drug products. The critical quality attributes associated with the process of HME are also discussed in this review. HME plays a significant role in the dosage form design, and the same has been mentioned with suitable examples. The role of HME in developing several sustained release formulations, films, and implants is described along with the research carried out in a similar domain.

Methods: The method includes the collection of data from different search engines like PubMed, ScienceDirect, and SciFinder to get coverage of relevant literature for accumulating appropriate information regarding HME, its importance in pharmaceutical product development, and advanced applications.

Results: HME is known to have advanced pharmaceutical applications in the domains related to 3D printing, nanotechnology, and PAT technology. HME-based technologies explored using Design-of- Experiments also lead to the systematic development of pharmaceutical formulations.

Conclusion: HME remains an adaptable and differentiated technique for overall formulation development.

背景:热熔挤压(HME)技术在不使用溶剂的情况下将高疏水性结晶药物转化为无定形固体方面显示出巨大的潜力。本文对HME过程中涉及的一般问题、HME的应用和进展进行了详细的探讨。目的:综述了与HME工艺相关的聚合物的理化性质。聚合物筛选的理论方法被强调为成功的HME加工药物产品的一部分。本文还讨论了与HME过程相关的关键质量属性。HME在剂型设计中起着重要的作用,并以合适的实例进行了介绍。HME在开发几种缓释制剂、薄膜和植入物中的作用,以及在类似领域进行的研究。方法:从PubMed、ScienceDirect、SciFinder等不同的搜索引擎中收集数据,覆盖相关文献,积累关于HME、HME在医药产品开发中的重要性和高级应用的适当信息。结果:已知HME在与3D打印,纳米技术和PAT技术相关的领域具有先进的制药应用。利用实验设计探索的基于hme的技术也导致了药物配方的系统开发。结论:HME仍然是一种适应性强、差异化强的整体处方开发技术。
{"title":"Recent Progress in Hot Melt Extrusion Technology in Pharmaceutical Dosage Form Design.","authors":"Sagar Salave,&nbsp;Kedar Prayag,&nbsp;Dhwani Rana,&nbsp;Prakash Amate,&nbsp;Rupali Pardhe,&nbsp;Ajinkya Jadhav,&nbsp;Anil B Jindal,&nbsp;Derajram Benival","doi":"10.2174/2667387816666220819124605","DOIUrl":"https://doi.org/10.2174/2667387816666220819124605","url":null,"abstract":"<p><strong>Background: </strong>The Hot Melt Extrusion (HME) technique has shown tremendous potential in transforming highly hydrophobic crystalline drug substances into amorphous solids without using solvents. This review explores in detail the general considerations involved in the process of HME, its applications and advances.</p><p><strong>Objective: </strong>The present review examines the physicochemical properties of polymers pertinent to the HME process. Theoretical approaches for the screening of polymers are highlighted as a part of successful HME processed drug products. The critical quality attributes associated with the process of HME are also discussed in this review. HME plays a significant role in the dosage form design, and the same has been mentioned with suitable examples. The role of HME in developing several sustained release formulations, films, and implants is described along with the research carried out in a similar domain.</p><p><strong>Methods: </strong>The method includes the collection of data from different search engines like PubMed, ScienceDirect, and SciFinder to get coverage of relevant literature for accumulating appropriate information regarding HME, its importance in pharmaceutical product development, and advanced applications.</p><p><strong>Results: </strong>HME is known to have advanced pharmaceutical applications in the domains related to 3D printing, nanotechnology, and PAT technology. HME-based technologies explored using Design-of- Experiments also lead to the systematic development of pharmaceutical formulations.</p><p><strong>Conclusion: </strong>HME remains an adaptable and differentiated technique for overall formulation development.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40626198","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
3D-Printed Microfluidics Potential in Combating Future and Current Pandemics (COVID-19). 3d打印微流体在对抗未来和当前流行病(COVID-19)中的潜力。
Pub Date : 2022-01-01 DOI: 10.2174/2667387816666220727101214
Heba A Eassa, Nada A Helal, Ahmed M Amer, Aliaa Fouad, Asser F Bedair, Reem Nagib, Ihab Mansoor, Motaz Hawash, Maha Abdul-Latif, Kamilia H A Mohammed, Mohamed A Helal, Mohamed Ismail Nounou

Coronavirus disease (COVID-19) emerged in China in December 2019. In March 2020, the WHO declared it a pandemic leading to worldwide lockdowns and travel restrictions. By May, it infected 4,789,205 and killed 318,789 people. This led to severe shortages in the medical sector besides devastating socio-economic effects. Many technologies such as artificial intelligence (AI), virtual reality (VR), microfluidics, 3D printing, and 3D scanning can step into contain the virus and hinder its extensive spread. This article aims to explore the potentials of 3D printing and microfluidic in accelerating the diagnosis and monitoring of the disease and fulfilling the shortages of personal protective equipment (PPE) and medical equipment. It highlights the main applications of 3D printers and microfluidics in providing PPE (masks, respirators, face shields, goggles, and isolation chambers/hoods), supportive care (respiratory equipment) and diagnostic supplies (sampling swabs & lab-on-chip) to ease the COVID-19 pressures. Also, the cost of such technology and regulation considerations are addressed. We conclude that 3D printing provided reusable and low-cost solutions to mitigate the shortages. However, safety, sterility, and compatibility with environmental protection standards need to be guaranteed through standardization and assessment by regulatory bodies. Finally, lessons learned from this pandemic can also help the world prepare for upcoming outbreaks.

2019年12月,中国出现新型冠状病毒病(COVID-19)。2020年3月,世界卫生组织宣布其为大流行,导致全球封锁和旅行限制。到5月,感染人数为4,789,205人,死亡人数为318,789人。这除了造成毁灭性的社会经济影响外,还导致医疗部门严重短缺。人工智能(AI)、虚拟现实(VR)、微流体、3D打印、3D扫描等许多技术都可以介入遏制病毒并阻止其广泛传播。本文旨在探讨3D打印和微流控技术在加速疾病诊断和监测以及弥补个人防护装备和医疗设备短缺方面的潜力。它强调了3D打印机和微流体在提供个人防护装备(口罩、呼吸器、面罩、护目镜和隔离室/头罩)、支持性护理(呼吸设备)和诊断用品(取样拭子和芯片实验室)方面的主要应用,以缓解COVID-19的压力。此外,还讨论了此类技术的成本和监管方面的考虑。我们的结论是,3D打印提供了可重复使用和低成本的解决方案,以缓解短缺。然而,安全性、无菌性和与环保标准的兼容性需要通过监管机构的标准化和评估来保证。最后,从这次大流行中吸取的教训也可以帮助世界为即将到来的疫情做好准备。
{"title":"3D-Printed Microfluidics Potential in Combating Future and Current Pandemics (COVID-19).","authors":"Heba A Eassa,&nbsp;Nada A Helal,&nbsp;Ahmed M Amer,&nbsp;Aliaa Fouad,&nbsp;Asser F Bedair,&nbsp;Reem Nagib,&nbsp;Ihab Mansoor,&nbsp;Motaz Hawash,&nbsp;Maha Abdul-Latif,&nbsp;Kamilia H A Mohammed,&nbsp;Mohamed A Helal,&nbsp;Mohamed Ismail Nounou","doi":"10.2174/2667387816666220727101214","DOIUrl":"https://doi.org/10.2174/2667387816666220727101214","url":null,"abstract":"<p><p>Coronavirus disease (COVID-19) emerged in China in December 2019. In March 2020, the WHO declared it a pandemic leading to worldwide lockdowns and travel restrictions. By May, it infected 4,789,205 and killed 318,789 people. This led to severe shortages in the medical sector besides devastating socio-economic effects. Many technologies such as artificial intelligence (AI), virtual reality (VR), microfluidics, 3D printing, and 3D scanning can step into contain the virus and hinder its extensive spread. This article aims to explore the potentials of 3D printing and microfluidic in accelerating the diagnosis and monitoring of the disease and fulfilling the shortages of personal protective equipment (PPE) and medical equipment. It highlights the main applications of 3D printers and microfluidics in providing PPE (masks, respirators, face shields, goggles, and isolation chambers/hoods), supportive care (respiratory equipment) and diagnostic supplies (sampling swabs & lab-on-chip) to ease the COVID-19 pressures. Also, the cost of such technology and regulation considerations are addressed. We conclude that 3D printing provided reusable and low-cost solutions to mitigate the shortages. However, safety, sterility, and compatibility with environmental protection standards need to be guaranteed through standardization and assessment by regulatory bodies. Finally, lessons learned from this pandemic can also help the world prepare for upcoming outbreaks.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40636945","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Differential Drug Release Kinetics from Paclitaxel-Loaded Polydioxanone Membranes and Capsules. 紫杉醇载聚二氧环酮膜和胶囊的差异药物释放动力学。
Pub Date : 2022-01-01 DOI: 10.2174/2667387816666220707143330
Smrithi Padmakumar, Merin Mary Varghese, Deepthy Menon

Background: Drug laden implantable systems can provide drug release over several hours to years, which eventually aid in the therapy of both acute and chronic diseases. The present study focuses on a fundamental evaluation of the influence of implant properties such as morphology, architecture, porosity, surface area, and wettability in regulating the drug release kinetics from drug-loaded polymeric matrices.

Methods: For this, Polydioxanone (PDS) was selected as the polymer and Paclitaxel (Ptx) as the model drug. Two different forms of the matrix implants, viz., reservoir type capsules developed by dip coating and matrix type membranes fabricated by phase inversion and electrospinning, were utilized for the study. Drug release from all the four different matrices prepared by simple techniques was evaluated in vitro in PBS and ex vivo in peritoneal wash fluid for ~4 weeks. The drug release profiles were thereafter correlated with the physicochemical parameters of the polymeric implants.

Results: Reservoir-type capsules followed a slow and steady zero-order kinetics, while matrix-type electrospun and phase inversion membranes displayed typical biphasic kinetics.

Conclusion: It was inferred that the slow degradation rate of PDS polymer as well as the implant properties like porosity and wettability play an important role in controlling the drug release rates.

背景:满载药物的植入式系统可以提供几个小时到几年的药物释放,最终有助于急性和慢性疾病的治疗。本研究的重点是对植入物的形态、结构、孔隙度、表面积和润湿性等特性在调节载药聚合物基质的药物释放动力学中的影响进行基本评估。方法:以聚二氧环酮(PDS)为聚合物,紫杉醇(Ptx)为模型药物。研究中采用了两种不同形式的基质植入物,即浸渍涂层制备的储层型胶囊和相转化和静电纺丝制备的基质型膜。用简单方法制备的四种不同基质在体外PBS和体外腹膜洗液中释放约4周。药物释放谱随后与聚合物植入物的理化参数相关。结果:储层型膜具有缓慢稳定的零级动力学,而基质型电纺丝膜和相转化膜具有典型的双相动力学。结论:推测PDS聚合物的缓慢降解速率以及植入物的孔隙度、润湿性等特性对药物释放率起重要控制作用。
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引用次数: 0
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Recent advances in drug delivery and formulation
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