ABSTRACT Solid lipid nanoparticles (SLN™) are a new generation of drug delivery systems being exp... more ABSTRACT Solid lipid nanoparticles (SLN™) are a new generation of drug delivery systems being exploited for several drugs since the nineties. These particles can be composed of different types of solid lipids, such as glycerides, waxes, and fatty acids, and stabilized by a wide range of surfactants. In the present chapter, the chemical structure, production methodology, and physicochemical characterization are systematically discussed. Parameters such as particle size, distribution, polymorphic behaviour, and crystallization are required to characterize SLN and may predict their in vitro stability and in vivo profile, therefore structural parameters can influence the biopharmaceutical properties. The use of SLN for drug delivery is also dependent on their toxicological profile in vitro. Nanotoxicology is also discussed addressing the key points that may limit the clinical use of SLN.
Abstract The word “cancer” is generically used to identify a wide range of diseases that are mali... more Abstract The word “cancer” is generically used to identify a wide range of diseases that are malignant tumors. Malignant tumors are of very different types, with different existing causes, evolutions, and thus with different treatments for each type. However, there is one feature that is common to all tumors: the division and uncontrolled growth of cells. The causes of cancer are not fully known, however, the modification of DNA appears to be responsible for the alteration of normal cell growth. Some chemicals can also induce the formation of cancerous tumors. In recent times, there has been considerable progress in the development of therapeutic drugs that act specifically on detectable molecular abnormalities in certain tumors, minimizing damage to normal cells. The prognosis for patients with cancer is influenced by the type of cancer; however, the grading and the presence of specific molecular markers can also bring benefits to establish the prognosis and determining individual treatments. This chapter focuses on the recent advances in nanobiomaterials (i.e., nanoparticles produced by biomaterials), used for the development of innovative approaches for oncology. Nanobiomaterials may be applied for cancer treatment either by passive or active pathways. In the passive pathway, nanoparticles circulate in the bloodstream and are accumulated into the tumor through enhanced permeability and retention effect; in the active pathway, nanoparticles reach the tumor through targeted drug therapy. Several types of biomaterials (e.g., lipids, phospholipids, polymers) may be used for the production of these nanoparticles, with specific size and surface electrical charge, and may even be surfaced with specific targeting ligands for site-specific targeting.
Abstract The central nervous system (CNS) barriers are essential boundaries that limit the intera... more Abstract The central nervous system (CNS) barriers are essential boundaries that limit the interaction with other peripheral systems, promoting CNS protection and neural integrity. Among them, the blood–brain barrier (BBB) is characterized by the intricate cellular architecture of its endothelium coupled with multiple specific transport systems that limit substance exchange in the brain’s vasculature. Neurodegenerative diseases such as Alzheimer and Parkinson diseases are, nowadays, high-incidence pathologies and all currently available treatments are mainly symptomatic and noncurative. Although the BBB is crucial in regulating CNS homeostasis, and essential for maintaining neuronal integrity, it limits drug delivery to the CNS. Therefore, the main challenge in developing new pharmaceutical alternatives for brain disease treatment is to deliver beneficial drugs across the BBB, while preventing the passage of potential neurotoxins. A nanotechnology-based approach has the potential to facilitate the transport of drugs across the BBB and to enhance their pharmacokinetic profile. The use of nanoparticle (NP) formulations able to encapsulate molecules with therapeutic value, while targeting specific biochemical processes in the brain, may enhance drug transport through the BBB in neurodegenerative disorders and target relevant regions in the brain for regenerative processes. In this chapter, we present a discussion based on the challenges that must be overcome to improve drug delivery to the CNS, focusing on recent advances in nanotechnology-based drug-delivery systems and how these systems and their potential effects could be exploited in the treatment of neurodegenerative diseases.
Abstract Psoriasis vulgaris is a chronic inflammatory skin disease for which classic therapies in... more Abstract Psoriasis vulgaris is a chronic inflammatory skin disease for which classic therapies include topical application of corticosteroids, dithranol, vitamin D analogues, cyclosporine A, methotrexate, and acitretin, alone or in association with phototherapy. Biological treatments are also available and include IL-23 and IL-17 inhibition. To overcome the side effects of current therapeutic options, new drug delivery systems have been proposed, as they may contribute to enhance drug accumulation in the site of action, depending on the type of psoriatic lesions. This chapter discusses the pathophysiology of the disease, the different types of lesions and the available treatments. Classic drugs can be formulated in polymeric and lipid nanoparticles with improved therapeutic outcomes.
The authors would like to acknowledge the financial support received through the project M-ERA-NE... more The authors would like to acknowledge the financial support received through the project M-ERA-NET/0004/2015, from the Portuguese Science and Technology Foundation, Ministry of Science and Education through national funds, and cofinanced by FEDER, under the Partnership Agreement PT2020.
International Journal of Pharmaceutics, Apr 1, 2022
Age-related macular degeneration (AMD) is defined as a degenerative, progressive and multifactori... more Age-related macular degeneration (AMD) is defined as a degenerative, progressive and multifactorial disorder that affects the macula with a complex etiology. The retinal pigment epithelium is a monolayer of cells that has the function to separate the surface of the choroid from the neural retina that is involved in the signal transduction leading to vision. The blood-aqueous barrier and the blood retinal barrier limit the permeation of drugs into the retina and thereby reducing their efficacy. Triamcinolone acetonide (TA) is widely used as anti-inflammatory and immunomodulatory drug that promotes the inhibition of the inflammatory processes. The factors that stimulate or inhibit angiogenesis in AMD create a local balance that is responsible for the growth of sub-retinal neovascularization. In AMD, the main angiogenic stimulus is the vascular endothelial growth factor (VEGF). In this work, nanoemulsions with cationic surfactants (mono- and dicationic DABCO and quinuclidine) were produced to deliver TA, and were found to reduce the production of tumor necrosis factor alpha (TNF-α), which stimulates the choroidal neovascularization development by upregulating the VEGF production, and consequently decreased the VEGF levels. Our results support the potential use of mono- and dicationic DABCO and quinuclidine-based cationic nanoemulsions for the delivery of TA in the treatment of AMD.
: Hydrogels for the modified-release drug delivery systems are a continuously growing area of int... more : Hydrogels for the modified-release drug delivery systems are a continuously growing area of interest for the pharmaceutical industry. According to the global market, the profit resulting from the use of polymers in this area is projected to reach $31.4 million by 2027. This review discusses the recent advances in and perspectives of hydrogel in drug delivery systems for oral, parenteral, nasal, topical, and ophthalmic delivery. The search was conducted, in January 2021, in an extensive database to identify studies published from January 2010 to December 2020. We described the main characteristic of the polymers to obtain an ideal hydrogel for a specific route of administration and the formulations. It was concluded that the hydrogels are useful to decrease the number of doses and side effects, promote adhesion of patient, and enhance the bioavailability of the drugs, thus improving the safety and efficacy of the treatment.
ABSTRACT Solid lipid nanoparticles (SLN™) are a new generation of drug delivery systems being exp... more ABSTRACT Solid lipid nanoparticles (SLN™) are a new generation of drug delivery systems being exploited for several drugs since the nineties. These particles can be composed of different types of solid lipids, such as glycerides, waxes, and fatty acids, and stabilized by a wide range of surfactants. In the present chapter, the chemical structure, production methodology, and physicochemical characterization are systematically discussed. Parameters such as particle size, distribution, polymorphic behaviour, and crystallization are required to characterize SLN and may predict their in vitro stability and in vivo profile, therefore structural parameters can influence the biopharmaceutical properties. The use of SLN for drug delivery is also dependent on their toxicological profile in vitro. Nanotoxicology is also discussed addressing the key points that may limit the clinical use of SLN.
Abstract The word “cancer” is generically used to identify a wide range of diseases that are mali... more Abstract The word “cancer” is generically used to identify a wide range of diseases that are malignant tumors. Malignant tumors are of very different types, with different existing causes, evolutions, and thus with different treatments for each type. However, there is one feature that is common to all tumors: the division and uncontrolled growth of cells. The causes of cancer are not fully known, however, the modification of DNA appears to be responsible for the alteration of normal cell growth. Some chemicals can also induce the formation of cancerous tumors. In recent times, there has been considerable progress in the development of therapeutic drugs that act specifically on detectable molecular abnormalities in certain tumors, minimizing damage to normal cells. The prognosis for patients with cancer is influenced by the type of cancer; however, the grading and the presence of specific molecular markers can also bring benefits to establish the prognosis and determining individual treatments. This chapter focuses on the recent advances in nanobiomaterials (i.e., nanoparticles produced by biomaterials), used for the development of innovative approaches for oncology. Nanobiomaterials may be applied for cancer treatment either by passive or active pathways. In the passive pathway, nanoparticles circulate in the bloodstream and are accumulated into the tumor through enhanced permeability and retention effect; in the active pathway, nanoparticles reach the tumor through targeted drug therapy. Several types of biomaterials (e.g., lipids, phospholipids, polymers) may be used for the production of these nanoparticles, with specific size and surface electrical charge, and may even be surfaced with specific targeting ligands for site-specific targeting.
Abstract The central nervous system (CNS) barriers are essential boundaries that limit the intera... more Abstract The central nervous system (CNS) barriers are essential boundaries that limit the interaction with other peripheral systems, promoting CNS protection and neural integrity. Among them, the blood–brain barrier (BBB) is characterized by the intricate cellular architecture of its endothelium coupled with multiple specific transport systems that limit substance exchange in the brain’s vasculature. Neurodegenerative diseases such as Alzheimer and Parkinson diseases are, nowadays, high-incidence pathologies and all currently available treatments are mainly symptomatic and noncurative. Although the BBB is crucial in regulating CNS homeostasis, and essential for maintaining neuronal integrity, it limits drug delivery to the CNS. Therefore, the main challenge in developing new pharmaceutical alternatives for brain disease treatment is to deliver beneficial drugs across the BBB, while preventing the passage of potential neurotoxins. A nanotechnology-based approach has the potential to facilitate the transport of drugs across the BBB and to enhance their pharmacokinetic profile. The use of nanoparticle (NP) formulations able to encapsulate molecules with therapeutic value, while targeting specific biochemical processes in the brain, may enhance drug transport through the BBB in neurodegenerative disorders and target relevant regions in the brain for regenerative processes. In this chapter, we present a discussion based on the challenges that must be overcome to improve drug delivery to the CNS, focusing on recent advances in nanotechnology-based drug-delivery systems and how these systems and their potential effects could be exploited in the treatment of neurodegenerative diseases.
Abstract Psoriasis vulgaris is a chronic inflammatory skin disease for which classic therapies in... more Abstract Psoriasis vulgaris is a chronic inflammatory skin disease for which classic therapies include topical application of corticosteroids, dithranol, vitamin D analogues, cyclosporine A, methotrexate, and acitretin, alone or in association with phototherapy. Biological treatments are also available and include IL-23 and IL-17 inhibition. To overcome the side effects of current therapeutic options, new drug delivery systems have been proposed, as they may contribute to enhance drug accumulation in the site of action, depending on the type of psoriatic lesions. This chapter discusses the pathophysiology of the disease, the different types of lesions and the available treatments. Classic drugs can be formulated in polymeric and lipid nanoparticles with improved therapeutic outcomes.
The authors would like to acknowledge the financial support received through the project M-ERA-NE... more The authors would like to acknowledge the financial support received through the project M-ERA-NET/0004/2015, from the Portuguese Science and Technology Foundation, Ministry of Science and Education through national funds, and cofinanced by FEDER, under the Partnership Agreement PT2020.
International Journal of Pharmaceutics, Apr 1, 2022
Age-related macular degeneration (AMD) is defined as a degenerative, progressive and multifactori... more Age-related macular degeneration (AMD) is defined as a degenerative, progressive and multifactorial disorder that affects the macula with a complex etiology. The retinal pigment epithelium is a monolayer of cells that has the function to separate the surface of the choroid from the neural retina that is involved in the signal transduction leading to vision. The blood-aqueous barrier and the blood retinal barrier limit the permeation of drugs into the retina and thereby reducing their efficacy. Triamcinolone acetonide (TA) is widely used as anti-inflammatory and immunomodulatory drug that promotes the inhibition of the inflammatory processes. The factors that stimulate or inhibit angiogenesis in AMD create a local balance that is responsible for the growth of sub-retinal neovascularization. In AMD, the main angiogenic stimulus is the vascular endothelial growth factor (VEGF). In this work, nanoemulsions with cationic surfactants (mono- and dicationic DABCO and quinuclidine) were produced to deliver TA, and were found to reduce the production of tumor necrosis factor alpha (TNF-α), which stimulates the choroidal neovascularization development by upregulating the VEGF production, and consequently decreased the VEGF levels. Our results support the potential use of mono- and dicationic DABCO and quinuclidine-based cationic nanoemulsions for the delivery of TA in the treatment of AMD.
: Hydrogels for the modified-release drug delivery systems are a continuously growing area of int... more : Hydrogels for the modified-release drug delivery systems are a continuously growing area of interest for the pharmaceutical industry. According to the global market, the profit resulting from the use of polymers in this area is projected to reach $31.4 million by 2027. This review discusses the recent advances in and perspectives of hydrogel in drug delivery systems for oral, parenteral, nasal, topical, and ophthalmic delivery. The search was conducted, in January 2021, in an extensive database to identify studies published from January 2010 to December 2020. We described the main characteristic of the polymers to obtain an ideal hydrogel for a specific route of administration and the formulations. It was concluded that the hydrogels are useful to decrease the number of doses and side effects, promote adhesion of patient, and enhance the bioavailability of the drugs, thus improving the safety and efficacy of the treatment.
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