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Book
Transmucosal Absorption Enhancers in the Drug Delivery Field
Authors: --- ---
ISBN: 3039218492 3039218484 Year: 2020 Publisher: MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

Development of strategies to assist the movement of poorly permeable molecules across biological barriers has long been the goal of drug delivery science. In the last three decades, there has been an exponential increase in advanced drug delivery systems that aim to address this issue. However, most proprietary delivery technologies that have progressed to clinical development are based on permeation enhancers (PEs) that have a history of safe use in man. This Special Issue entitled “Transmucosal Absorption Enhancers in the Drug Delivery Field” aims to present the current state-of-the-art in the application of PEs to improve drug absorption. Emphasis is placed on identification of novel permeation enhancers, mechanisms of barrier alteration, physicochemical properties of PEs that contribute to optimal enhancement action, new delivery models to assess PEs, studies assessing safety of PEs, approaches to assist translation of PEs into effective oral, nasal, ocular and vaginal dosage forms and combining PEs with other delivery strategies.

Keywords

chitosan --- intestinal epithelial cells --- ocular delivery --- amphiphilic polymers --- cornea --- tight junction modulator --- cyclodextrin --- permeability --- gemini surfactant --- transferrin --- compound 48/80 --- epithelial permeability --- cervicovaginal tumors --- nanoparticles --- confocal laser scanning microscopy --- safety --- formulation --- salcaprozate sodium --- intestinal absorption --- FITC-dextran --- curcumin --- block copolymers --- nasal vaccination --- whole leaf --- brush border --- ocular drug delivery --- vaccine adjuvant --- nanoparticle --- nasal delivery --- efflux --- permeation enhancers --- absorption enhancers --- nose to brain delivery --- small intestine --- epithelium --- CNS disorders --- absorption modifying excipients --- insulin --- absorption enhancer --- gel --- intestinal delivery --- thermogel system --- Caco-2 --- biocompatibility studies --- absorption enhancement --- man --- PN159 --- poorly absorbed drug --- tryptophan --- tight junction --- oral macromolecule delivery --- penetration enhancer --- intestinal permeation enhancers --- nanocrystals --- simvastatin --- nanomedicine --- enterocyte --- N-dodecyl-?-D-maltoside (DDM) --- cell-penetrating peptide --- quaternization --- KLAL --- nasal --- nasal permeability --- transmucosal drug delivery --- Caco-2 cells --- mast cell activator --- penetration enhancers --- drug delivery --- nose-to-brain --- bioenhancer --- polymeric micelles --- mucoadhesion --- cell-penetrating peptide (CPP) --- simulated intestinal fluid --- vaginal delivery --- nasal formulation --- pharmacokinetic interaction --- sodium caprate --- clinical trial --- transmucosal permeation --- drug absorption enhancer --- sugar-based surfactants --- nanocapsules --- imatinib --- teriparatide --- osteoporosis --- hydrophobization --- F-actin --- combined microsphere --- transepithelial electrical resistance --- oral delivery --- ocular conditions --- metabolism --- antimicrobial peptide --- permeation enhancer --- drug administration --- antiepileptic drug --- amino acid --- in vivo studies --- sodium cholate (NaC) --- epithelial transport --- preclinical --- nose to brain transport --- pharmacokinetics --- chitosan derivatives --- ophthalmology --- tight junctions --- sheep --- cationic functionalization --- GLP-1 --- pulmonary --- and liposome --- cytochrome P450 --- claudin --- P-glycoprotein --- in situ hydrogel --- mucoadhesiveness --- PTH 1-34 --- Aloe vera --- oral peptides


Book
Preclinical Evaluation of Lipid-Based Nanosystems
Authors: ---
Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

The use of lipid-based nanosystems, including lipid nanoparticles (solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC)), nanoemulsions, and liposomes, among others, is widespread. Several researchers have described the advantages of different applications of these nanosystems. For instance, they can increase the targeting and bioavailability of drugs, improving therapeutic effects. Their use in the cosmetic field is also promising, owing to their moisturizing properties and ability to protect labile cosmetic actives. Thus, it is surprising that only a few lipid-based nanosystems have reached the market. This can be explained by the strict regulatory requirements of medicines and the occurrence of unexpected in vivo failure, which highlights the need to conduct more preclinical studies.Current research is focused on testing the in vitro, ex vivo, and in vivo efficacy of lipid-based nanosystems to predict their clinical performance. However, there is a lack of method validation, which compromises the comparison between different studies.This book brings together the latest research and reviews that report on in vitro, ex vivo, and in vivo preclinical studies using lipid-based nanosystems. Readers can find up-to-date information on the most common experiments performed to predict the clinical behavior of lipid-based nanosystems. A series of 15 research articles and a review are presented, with authors from 15 different countries, which demonstrates the universality of the investigations that have been carried out in this area.

Keywords

Technology: general issues --- nanostructured lipid carriers (NLC) --- formulation optimization --- rivastigmine --- quality by design (QbD) --- nasal route --- nose-to-brain --- N-alkylisatin --- liposome --- urokinase plasminogen activator --- PAI-2 --- SerpinB2 --- breast cancer --- liposomes --- target delivery nanosystem --- FZD10 protein --- colon cancer therapy --- supersaturation --- silica-lipid hybrid --- spray drying --- lipolysis --- lipid-based formulation --- fenofibrate --- mesoporous silica --- oral drug delivery --- hyaluronic acid --- drug release --- light activation --- stability --- mobility --- biocorona --- dissolution enhancement --- phospholipids --- solid dosage forms --- porous microparticles --- nanoemulsion(s) --- phase-behavior --- DoE --- D-optimal design --- vegetable oils --- non-ionic surfactants --- efavirenz --- flaxseed oil --- nanostructured lipid carriers --- nanocarrier --- docohexaenoic acid --- neuroprotection --- neuroinflammation --- fluconazole --- Box‒Behnken design --- nanotransfersome --- ulcer index --- zone of inhibition --- rheological behavior --- ex vivo permeation --- nanomedicine --- cancer --- doxorubicin --- melanoma --- drug delivery --- ultrasound contrast agents --- phospholipid coating --- ligand distribution --- cholesterol --- acoustic response --- microbubble --- lipid phase --- dialysis --- ammonia --- intoxication --- cyanocobalamin --- vitamin B12 --- atopic dermatitis --- psoriasis --- transferosomes --- lipid vesicles --- skin topical delivery --- oligonucleotide --- self-emulsifying drug delivery systems --- hydrophobic ion pairing --- intestinal permeation enhancers --- Caco-2 monolayer --- clarithromycin --- solid lipid nanoparticles --- optimization --- permeation --- pharmacokinetics --- follicular targeting --- dexamethasone --- alopecia areata --- lipomers --- lipid polymer hybrid nanocapsules --- biodistribution --- skin --- ethyl cellulose --- nanostructured lipid carriers (NLC) --- formulation optimization --- rivastigmine --- quality by design (QbD) --- nasal route --- nose-to-brain --- N-alkylisatin --- liposome --- urokinase plasminogen activator --- PAI-2 --- SerpinB2 --- breast cancer --- liposomes --- target delivery nanosystem --- FZD10 protein --- colon cancer therapy --- supersaturation --- silica-lipid hybrid --- spray drying --- lipolysis --- lipid-based formulation --- fenofibrate --- mesoporous silica --- oral drug delivery --- hyaluronic acid --- drug release --- light activation --- stability --- mobility --- biocorona --- dissolution enhancement --- phospholipids --- solid dosage forms --- porous microparticles --- nanoemulsion(s) --- phase-behavior --- DoE --- D-optimal design --- vegetable oils --- non-ionic surfactants --- efavirenz --- flaxseed oil --- nanostructured lipid carriers --- nanocarrier --- docohexaenoic acid --- neuroprotection --- neuroinflammation --- fluconazole --- Box‒Behnken design --- nanotransfersome --- ulcer index --- zone of inhibition --- rheological behavior --- ex vivo permeation --- nanomedicine --- cancer --- doxorubicin --- melanoma --- drug delivery --- ultrasound contrast agents --- phospholipid coating --- ligand distribution --- cholesterol --- acoustic response --- microbubble --- lipid phase --- dialysis --- ammonia --- intoxication --- cyanocobalamin --- vitamin B12 --- atopic dermatitis --- psoriasis --- transferosomes --- lipid vesicles --- skin topical delivery --- oligonucleotide --- self-emulsifying drug delivery systems --- hydrophobic ion pairing --- intestinal permeation enhancers --- Caco-2 monolayer --- clarithromycin --- solid lipid nanoparticles --- optimization --- permeation --- pharmacokinetics --- follicular targeting --- dexamethasone --- alopecia areata --- lipomers --- lipid polymer hybrid nanocapsules --- biodistribution --- skin --- ethyl cellulose


Book
Brain-Targeted Drug Delivery
Author:
ISBN: 3036552812 3036552820 Year: 2022 Publisher: MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

Brain diseases currently affect one in six people worldwide; they include a wide range of neurological diseases, from Alzheimer’s and Parkinson’s diseases to epilepsy, brain injuries, brain cancer, neuroinfections, and strokes. The treatment of these diseases is complex and limited due to the presence of the blood–brain barrier (BBB), which covers the entirety of the brain. The BBB not only has the function of protecting the brain from harmful substances; it is also a metabolic barrier and a transport regulator of nutrients/serum factors/neurotoxins. Knowing these characteristics when it comes to the treatment of brain diseases makes it easier to understand the lack of efficacy of therapeutic drugs, resulting from the innate resistance of the BBB to permeation. To overcome this limitation, drug delivery systems based on nanotechnology/microtechnology have been developed. Brain-targeted drug delivery enables targeted therapy with a higher therapeutic efficacy and fewer side effects because it targets moieties present in the drug delivery systems.

Keywords

Technology: general issues --- drug delivery into the brain --- transendothelium based on receptor-mediated transcytosis --- immunotherapy --- Alzheimer’s disease --- anti-tau and anti-receptor bispecific monoclonal antibodies --- Alzheimer’s disease-relevant tau species --- temporal-spatial pathological Aβ and tau distribution --- interactions between Aβ and tau --- tau clearance in microglia --- tau clearance in neurons --- liposome --- nanoparticle --- seizure --- laser --- ultrasound --- naringenin --- nanostructured lipid carrier --- intranasal delivery --- central composite rotatable design --- depression --- pomegranate seed oil --- nasal delivery system --- memory impairment --- movement impairment --- delivery to brain --- improved memory --- phospholipid oily gel --- high-grade glioma --- diffuse midline glioma --- glioblastoma --- IL-13Rα2 --- IL-13 --- immunotoxin --- targeted therapy --- GB-13 --- IL13.E13K-PE4E --- receptor expression --- acetaminophen --- blood–brain barrier --- claudin-5 --- CNS drug delivery --- opioids --- tight junction --- microdialysis --- cerebral open flow microperfusion --- electrochemical biosensors --- macromolecules --- tolcapone --- microparticles --- nanoparticles --- PLGA --- Parkinson’s disease --- nose to brain delivery --- gene therapy --- polyplexes --- hyaluronidase --- glycol chitosan --- brain cancer --- chemoattractant --- CXCL --- CXCR --- glioblastoma multiforme --- 3D cell culture systems --- non-human primate --- convection-enhanced delivery --- neurosurgery --- optogenetics --- blood-brain barrier --- brain targeted therapy --- drug delivery --- cerebrospinal fluid microcirculation --- brain biodistribution --- n/a --- Alzheimer's disease --- Alzheimer's disease-relevant tau species --- Parkinson's disease


Book
Current Insights on Lipid-Based Nanosystems
Authors: --- ---
ISBN: 303656165X 3036561668 Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

Lipid-based nanosystems, including solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), cationic lipid nanoparticles, nanoemulsions, and liposomes, have been extensively studied to improve drug delivery through different administration routes. The main advantages of these systems are their ability to protect, transport, and control the release of lipophilic and hydrophilic molecules (either small-molecular-weight molecules or macromolecules); the use of generally recognized as safe (GRAS) excipients that minimize the toxicity of the formulations; and the possibility to modulate pharmacokinetics and enable the site-specific delivery of encapsulated payloads. In addition, the versatility of lipid-based nanosystems has further been demonstrated for the delivery of vaccines, the protection of active cosmetic ingredients, and the improvement of moisturizing properties of cosmetic formulations.Lipid-based nanosystems are well established and there are already different commercially approved formulations for various human disorders. This success has paved the way for the diversification of the pipeline of development, to address unmet medical needs for several indications, such as cancer, neurological disorders, and autoimmune, genetic, and infectious diseases.This Special Issue aims to update readers on the latest research on lipid-based nanosystems, both at the preclinical and clinical levels. A series of 15 articles (six reviews and nine studies) is presented, with authors from 12 different countries, showing the globality of the investigations that are being carried out in this area.

Keywords

Technology: general issues --- Echinococcus granulosus --- scolicidal --- nanoliposome --- juglone --- apoptotic activity --- hydrogel --- SLNs --- nose-to-brain delivery --- mucoadhesion --- quality by design --- antioxidant activity --- nasal administration --- nanostructured lipid carriers --- solid lipid nanoparticles --- in vitro cell cultures --- 3D nasal casts --- lung cancer --- targeted drug delivery --- lipid-based nanocarriers --- pulmonary delivery --- dry powder inhalers --- aerosols --- liposomes --- nanoemulsions --- nanotechnology --- biologically active compounds --- dermal drug delivery --- polyphenols --- phytophenols --- skin permeation --- chemotherapy --- radiotherapy --- active targeting --- passive targeting --- tumor --- immunoconjugate --- traditional liposome --- stealth liposome --- triggered release --- limitations of liposomes --- drug transfer --- in vitro release --- colloidal drug carriers --- lipid nanoparticles --- hydrogel beads --- cholesteryl nonanoate --- bovine serum albumin --- skin diseases --- lipid-based nanosystems --- cream --- ointment --- gel --- pH-sensitive --- liposome --- imidazole --- anticancer --- drug delivery --- multicellular spheroids --- dapagliflozin --- Box–Behnken design --- FTIR --- DSC --- XRD --- SEM --- AFM --- in vitro Franz diffusion cells --- lipid-based nanoparticles --- nanocarrier --- surface charge --- delivery systems --- chronic treatment --- mice --- anti-oxidant activity --- hepatoprotective effect --- phospholipid --- phytosomes --- Silymarin --- Colorectal Cancer --- Niosomes --- Oxaliplatin --- Paclitaxel --- d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) --- therapeutic nucleic acids --- schizophrenia --- quetiapine fumarate --- glycerosomes --- central composite rotatable design --- bioavailability --- pharmacokinetic --- n/a --- Box-Behnken design


Book
Preclinical Evaluation of Lipid-Based Nanosystems
Authors: ---
Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

The use of lipid-based nanosystems, including lipid nanoparticles (solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC)), nanoemulsions, and liposomes, among others, is widespread. Several researchers have described the advantages of different applications of these nanosystems. For instance, they can increase the targeting and bioavailability of drugs, improving therapeutic effects. Their use in the cosmetic field is also promising, owing to their moisturizing properties and ability to protect labile cosmetic actives. Thus, it is surprising that only a few lipid-based nanosystems have reached the market. This can be explained by the strict regulatory requirements of medicines and the occurrence of unexpected in vivo failure, which highlights the need to conduct more preclinical studies.Current research is focused on testing the in vitro, ex vivo, and in vivo efficacy of lipid-based nanosystems to predict their clinical performance. However, there is a lack of method validation, which compromises the comparison between different studies.This book brings together the latest research and reviews that report on in vitro, ex vivo, and in vivo preclinical studies using lipid-based nanosystems. Readers can find up-to-date information on the most common experiments performed to predict the clinical behavior of lipid-based nanosystems. A series of 15 research articles and a review are presented, with authors from 15 different countries, which demonstrates the universality of the investigations that have been carried out in this area.

Keywords

Technology: general issues --- nanostructured lipid carriers (NLC) --- formulation optimization --- rivastigmine --- quality by design (QbD) --- nasal route --- nose-to-brain --- N-alkylisatin --- liposome --- urokinase plasminogen activator --- PAI-2 --- SerpinB2 --- breast cancer --- liposomes --- target delivery nanosystem --- FZD10 protein --- colon cancer therapy --- supersaturation --- silica-lipid hybrid --- spray drying --- lipolysis --- lipid-based formulation --- fenofibrate --- mesoporous silica --- oral drug delivery --- hyaluronic acid --- drug release --- light activation --- stability --- mobility --- biocorona --- dissolution enhancement --- phospholipids --- solid dosage forms --- porous microparticles --- nanoemulsion(s) --- phase-behavior --- DoE --- D-optimal design --- vegetable oils --- non-ionic surfactants --- efavirenz --- flaxseed oil --- nanostructured lipid carriers --- nanocarrier --- docohexaenoic acid --- neuroprotection --- neuroinflammation --- fluconazole --- Box‒Behnken design --- nanotransfersome --- ulcer index --- zone of inhibition --- rheological behavior --- ex vivo permeation --- nanomedicine --- cancer --- doxorubicin --- melanoma --- drug delivery --- ultrasound contrast agents --- phospholipid coating --- ligand distribution --- cholesterol --- acoustic response --- microbubble --- lipid phase --- dialysis --- ammonia --- intoxication --- cyanocobalamin --- vitamin B12 --- atopic dermatitis --- psoriasis --- transferosomes --- lipid vesicles --- skin topical delivery --- oligonucleotide --- self-emulsifying drug delivery systems --- hydrophobic ion pairing --- intestinal permeation enhancers --- Caco-2 monolayer --- clarithromycin --- solid lipid nanoparticles --- optimization --- permeation --- pharmacokinetics --- follicular targeting --- dexamethasone --- alopecia areata --- lipomers --- lipid polymer hybrid nanocapsules --- biodistribution --- skin --- ethyl cellulose --- n/a


Book
Preclinical Evaluation of Lipid-Based Nanosystems
Authors: ---
Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

Loading...
Export citation

Choose an application

Bookmark

Abstract

The use of lipid-based nanosystems, including lipid nanoparticles (solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC)), nanoemulsions, and liposomes, among others, is widespread. Several researchers have described the advantages of different applications of these nanosystems. For instance, they can increase the targeting and bioavailability of drugs, improving therapeutic effects. Their use in the cosmetic field is also promising, owing to their moisturizing properties and ability to protect labile cosmetic actives. Thus, it is surprising that only a few lipid-based nanosystems have reached the market. This can be explained by the strict regulatory requirements of medicines and the occurrence of unexpected in vivo failure, which highlights the need to conduct more preclinical studies.Current research is focused on testing the in vitro, ex vivo, and in vivo efficacy of lipid-based nanosystems to predict their clinical performance. However, there is a lack of method validation, which compromises the comparison between different studies.This book brings together the latest research and reviews that report on in vitro, ex vivo, and in vivo preclinical studies using lipid-based nanosystems. Readers can find up-to-date information on the most common experiments performed to predict the clinical behavior of lipid-based nanosystems. A series of 15 research articles and a review are presented, with authors from 15 different countries, which demonstrates the universality of the investigations that have been carried out in this area.

Keywords

nanostructured lipid carriers (NLC) --- formulation optimization --- rivastigmine --- quality by design (QbD) --- nasal route --- nose-to-brain --- N-alkylisatin --- liposome --- urokinase plasminogen activator --- PAI-2 --- SerpinB2 --- breast cancer --- liposomes --- target delivery nanosystem --- FZD10 protein --- colon cancer therapy --- supersaturation --- silica-lipid hybrid --- spray drying --- lipolysis --- lipid-based formulation --- fenofibrate --- mesoporous silica --- oral drug delivery --- hyaluronic acid --- drug release --- light activation --- stability --- mobility --- biocorona --- dissolution enhancement --- phospholipids --- solid dosage forms --- porous microparticles --- nanoemulsion(s) --- phase-behavior --- DoE --- D-optimal design --- vegetable oils --- non-ionic surfactants --- efavirenz --- flaxseed oil --- nanostructured lipid carriers --- nanocarrier --- docohexaenoic acid --- neuroprotection --- neuroinflammation --- fluconazole --- Box‒Behnken design --- nanotransfersome --- ulcer index --- zone of inhibition --- rheological behavior --- ex vivo permeation --- nanomedicine --- cancer --- doxorubicin --- melanoma --- drug delivery --- ultrasound contrast agents --- phospholipid coating --- ligand distribution --- cholesterol --- acoustic response --- microbubble --- lipid phase --- dialysis --- ammonia --- intoxication --- cyanocobalamin --- vitamin B12 --- atopic dermatitis --- psoriasis --- transferosomes --- lipid vesicles --- skin topical delivery --- oligonucleotide --- self-emulsifying drug delivery systems --- hydrophobic ion pairing --- intestinal permeation enhancers --- Caco-2 monolayer --- clarithromycin --- solid lipid nanoparticles --- optimization --- permeation --- pharmacokinetics --- follicular targeting --- dexamethasone --- alopecia areata --- lipomers --- lipid polymer hybrid nanocapsules --- biodistribution --- skin --- ethyl cellulose --- n/a

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