Part 1 book “Drug delivery - An integrated clinical and engineering approach” has contents: An Introduction to key concepts in drug delivery, an introduction to pharmacokinetics, gastroretentive delivery, invasive versus noninvasive delivery of insulin, the artificial pancreas,… and other contents.
Drug Delivery An Integrated Clinical and Engineering Approach http://taylorandfrancis.com Drug Delivery An Integrated Clinical and Engineering Approach Edited by Yitzhak Rosen Pablo Gurman Noel M Elman The material in this book, whether related to medicine or any other topic, should be verified as to its accuracy, currency, and preciseness by the reader It should in no way replace any advice given by a medical professional or any other professional None of the information provided here should be a substitute for additional reading, advice, experience, or other relevant information in any topic discussed in this book CRC Press Taylor & Francis Group 6000 Broken Sound Parkway NW, Suite 300 Boca Raton, FL 33487-2742 © 2017 by Taylor & Francis Group, LLC CRC Press is an imprint of Taylor & Francis Group, an Informa business No claim to original U.S Government works Printed on acid-free paper Version Date: 20161109 International Standard Book Number-13: 978-1-4665-6594-4 (Hardback) This book contains information obtained from authentic and highly regarded sources Reasonable efforts have been made to publish reliable data and information, but the author and publisher cannot assume responsibility for the validity of all materials or the consequences of their use The authors and publishers have attempted to trace the copyright holders of all material reproduced in this publication and apologize to copyright holders if permission to publish in this form has not been obtained If any copyright material has not been acknowledged please write and let us know so we may rectify in any future reprint Except as permitted under U.S Copyright Law, no part of this book may be reprinted, reproduced, transmitted, or utilized in any form by any electronic, mechanical, or other means, now known or hereafter invented, including photocopying, microfilming, and recording, or in any information storage or retrieval system, without written permission from the publishers For permission to photocopy or use material electronically from this work, please access www.copyright com (http://www.copyright.com/) or contact the Copyright Clearance Center, Inc (CCC), 222 Rosewood Drive, Danvers, MA 01923, 978-750-8400 CCC is a not-for-profit organization that provides licenses and registration for a variety of users For organizations that have been granted a photocopy license by the CCC, a separate system of payment has been arranged Trademark Notice: Product or corporate names may be trademarks or registered trademarks, and are used only for identification and explanation without intent to infringe Visit the Taylor & Francis Web site at http://www.taylorandfrancis.com and the CRC Press Web site at http://www.crcpress.com Contents Foreword ix Acknowledgments xi Editors xiii Contributors xv Chapter An Introduction to Key Concepts in Drug Delivery Stephen Kuperberg, Mahyar Pourriahi, Jonathan Daich, Aaron Richler, Pablo Gurman, Noel M Elman, and Yitzhak Rosen Chapter An Introduction to Pharmacokinetics: From Conventional to Advanced Systemic Drug Delivery Systems 13 Alan Talevi, Luis Bruno Blanch, and Guillermo R Castro Chapter Transporter- and Enzyme-Targeted Prodrugs for Improved Oral Drug Delivery 47 Arik Dahan and Shimon Ben-Shabat Chapter Gastroretentive Delivery: Physicochemical, Biopharmaceutical, Technological, and Regulatory Considerations 65 Yuvraj Singh, Vivek K Pawar, Mohini Chaurasia, and Manish K Chourasia Chapter Invasive versus Noninvasive Delivery of Insulin 101 Sandra Soares, Ana Costa, Pedro Fonte, and Bruno Sarmento Chapter The Artificial Pancreas 147 Joseph Shivers, Jennifer Lane, Eyal Dassau, and Howard Zisser Chapter Micro/Nano Devices for Drug Delivery 181 Roya Sheybani and Ellis Meng Chapter Microneedle-Mediated Vaccines 207 Ryan F Donnelly, Maelíosa T C McCrudden, Sharifa Al-Zahrani, and Steven J Fallows v vi Contents Chapter Application of Nanoparticle Tracking Analysis in Drug Delivery 237 Matthew Wright Chapter 10 Microsponges for Drug Delivery 265 Rishabh Srivastava Chapter 11 Chitosan for Advancing Drug Delivery 293 Sanjay K Jain and Satish Shilpi Chapter 12 Gene Delivery by Electroporation 341 Julie Gehl Chapter 13 Drug Delivery Systems for Infectious Diseases 349 Maximiliano L Cacicedo, Germán A Islan, Pablo Gurman, and Guillermo R Castro Chapter 14 Nanotechnology in Drug Delivery to Chronic Inflammatory Diseases 373 Mazen M El-Hammadi and José L Arias Chapter 15 Intrathecal Drug Delivery 401 SriKrishna Chandran Chapter 16 Cancer Stem Cell Drug Delivery 411 Masturah Bte Mohd Abdul Rashid, Lissa Nurrul Abdullah, Tan Boon Toh, and Edward Kai-Hua Chow Chapter 17 Cardiac Drug Delivery 439 Paula Díaz-Herráez, Simón Pascual-Gil de Gómez, Elisa Garbayo, Teresa Simón-Yarza, Felipe Prósper, and María J Blanco-Prieto Chapter 18 Current Developments in Nanotherapeutics for Airway Diseases 481 Indrajit Roy, Ridhima Juneja, Komal Sethi, and Neeraj Vij vii Contents Chapter 19 Intravitreal Drug Delivery 495 Omar Saleh, Mark Ihnen, and Shlomit Schaal Chapter 20 Drug Delivery in Obstetrics and Gynecology 531 David Shveiky, Yael Hants, and Sarit Helman Chapter 21 Drug Delivery Systems: A Regulatory Perspective 549 Pablo Gurman, Noel M Elman, and Yitzhak Rosen Index 573 http://taylorandfrancis.com Foreword This book is a comprehensive overview in the much needed area of drug delivery It addresses a critical unmet need, the approach of integrating the clinical and engineering disciplines for drug delivery optimization and advancement This integration is a must, requires a patient-oriented approach, and is a key foundation in drug delivery development Furthermore, the book focuses on important advances and discusses how an integrated approach was used for these advances It consists of 21 chapters, starting with a thorough introduction to drug delivery and pharmacokinetics, followed by diverse clinical examples of this integration The book discusses the following areas and their advances: oral and intrathecal drug delivery; insulin delivery and artificial pancreas; micro- and nanotechnology for drug delivery, including applications of micro- and nanotechnology in vaccines; inflammatory diseases; airway diseases and the use of nanoparticles as tracking systems; biomaterial-based delivery systems, including chitosan and microsponges; gene delivery, cancer drug delivery with a focus on stem cells; cardiac drug delivery; intravitreal drug delivery; and drug delivery in obstetrics and gynecology as well as an important chapter on FDA regulation of drug delivery systems As an experienced clinician and discoverer of a new autoimmune syndrome (ASIA Syndrome), developer of novel therapeutics, publisher of numerous papers and books, and editor in chief of two journals on autoimmunity (Autoimmunity Reviews IF-7.95 and Journal of Autoimmunity IF 8.4), it is my hope that all clinicians and engineers involved in advancing drug delivery will find in this book a useful resource Therefore, I give this book the highest recommendation Yehuda Shoenfeld, MD, FRCP, MaACR Head of Zabludowicz Center for Autoimmune Diseases Sheba Medical Center, Affiliated with Tel Aviv University ix 250 Drug Delivery carriers in serum compared to un-PEGylated liposomes, which were shown to have faster kinetics of degradation Finally, Smith et al [51] have used NTA to show that the change in flux was not a result of a change in size due to aggregation of the hemoglobin at the different pHs tested when confirming that alginate hydrogel has a negative impact on in vitro collagen deposition by fibroblasts Encapsulation and Nanocarrier Production Some of the earliest studies incorporating NTA in the field of nanocarrier production included investigations into cholesteric and nematic emulsions [52] and binary microgel thin films [53] This led to further work where NTA was used to follow changes in size of nanocapsules for intestinal delivery and enhanced oral bioavailability of tacrolimus (a P-gp substrate) [54] as well as a range of other carriers [55–57] As described in the methodology section of this chapter, the lower limit of detection of NTA is often reached when materials with low light-scattering properties are characterized However, in spite of this property being present in micellar systems, Vakurov et al [58] successfully used the technology to characterize this type of structure This work was then built on as researchers looked at drug delivery micellar formulations for controlled release of covalently entrapped doxorubicin [59] and the encapsulation of mithramycin [60,61] These later studies demonstrated that microfluidics is a powerful technology for nanoprecipitation-based production of drug-loaded polymeric micelles as compared to batch systems since it enabled better control, reproducibility, and homogeneity of the size characteristics of the produced micelles The work by Pazik et al [62] looking at BaTiO3 explored the surface functional ization of the metal oxide nanoparticles with biologically active molecules containing phosphonate moieties A wealth of techniques were employed in the investigation, including SEM/energy dispersive spectroscopy, pH-metric titration, nuclear magnetic resonance (NMR) and infrared (IR) spectroscopy, dynamic light scattering, zeta potential, thermogravimetric analysis, and radiometric measurements with NTA aiding them to come to the conclusion that the application of amino phosphonic acids as surface ligands provided nanoparticles with considerable solution stability in an aqueous medium at neutral pH and especially in the presence of electrolytes, thus opening the broad prospect of applications for the thus produced nanoparticle dispersions in the domains of nano-optics and nanomagnetism Biosilicate nanoparticles formed by mimicking peptides using polyethyleneimine were fabricated and characterized by Neville et al [63] Using a combination of NTA and TEM, they characterized for the first time nanoparticles made from tetramethyl orthosilicate to entrap enzymes This work was built on and explained further in a recent report on the production and characterization of bioactive thiolsilicate nanoparticles [64] Zu et al [65] have also described the preparation of ultrafine polyethylene-silica composite particles with a core-shell structure using SEM observation and NTA to determine particle sphericity and a mean size of 160 nm, respectively Application of Nanoparticle Tracking Analysis in Drug Delivery 251 Sokolova et al [66] used the respective benefits of SEM, DLS, analytical ultracentrifugation, and NTA to analyze size, surface charge, and morphology of nanoparticles in their investigation into the dendritic cell maturation and T cell activation through the application of calcium phosphate nanoparticles encapsulating toll-like receptor ligands and the antigen hemagglutinin Similarly, recent developments of a nanoparticulate formulation of retinoic acid that suppresses Th17 cells and upregulates regulatory T cells employed NTA to measure particle size [67], and the stability of nanometer-sized prodrug (nanoprodrug) production by a spontaneous emulsification mechanism was confirmed by NTA to be constant at 120–140 nm in diameter [68] Geng et al [69] used NTA to establish that the development and characterizations of maleimide-functionalized biopolymer (Mal-PGA-Asp) as an effective targeted drug delivery carrier synthesized from an amidation reaction between aspartylated PGA (PGA-Asp) and N-(maleimidohexanoyl)-ethylenediamine (NME) led to significantly enhanced cellular uptake of TP13-Mal-PGA-Asp3-Pt in the human hepatoma cell line SMMC-7721 as shown by fluorescence imaging and flow cytometry NTA was used to show the biopolymer had an average size 87 ± 28 nm During attempts to improve the homogeneity of nanosized lipid vesicles made by constant pressure-controlled extrusion processes for use as drug delivery vehicles, NTA, DLS, and EM were all used to characterize the degree of polydispersity within the product [70] NTA was also used in determining the optimum formulation of albumin based theragnostic nanoparticles as a potential delivery system for tumor targeting, and when used in conjunction with DLS confirmed that the optimized nanoparticle formulation had a modal size of 125 nm [71] The counting capability of NTA was put to use in the study by Wrenn et al [72] as they looked at the number and size of liposomes when exposed to ultrasound in an initial attempt to distinguish mechanisms and quantify the relative contributions of liposome destruction versus diffusion through the bilayer It was shown that the overall number of liposomes decreased with an increase in ultrasound exposure time with nearly 50% of the reduction occurring within the first minutes of exposure This result strongly implied that some vesicle destruction occurs as a result of exposure, a view that is consistent with prior studies by the group Yandrapu et al [73] used NTA to characterize dendrimer conjugates in their study for the development of novel thiolated dendrimers for mucoadhesive drug delivery The study showed that their developed particles exhibited sustained release of acyclovir and higher levels of mucoadhesion In a study to develop curcumin-loaded lipid-core nanocapsules (C-LNC), in an attempt to improve the antiglioma activity of this polyphenol, visualization of the C-LNC was carried out by NTA The data obtained suggested that the nanoencapsulation of curcumin in LNC is an important strategy to improve its pharmacological efficacy in the treatment of gliomas [74] A recent set of experiments explored the effect of different relative humidity conditions on the stability of freeze-dried formulations containing trehalose or melibiose NTA was used to determine there to be a huge range polydisperisty with particle sizes starting at 50 nm and going up to 1000 nm [75] 252 Drug Delivery Using DLS and NTA to confirm formulation unimodal size distribution (with polydispersity value