Microneedle-based ocular drug delivery systems – recent advances and challenges

• Piotr Gadziński,
• Anna Froelich,
• Monika Wojtyłko,
• Antoni Białek,
• Julia Krysztofiak and
• Tomasz Osmałek

Beilstein J. Nanotechnol. 2022, 13, 1167–1184, doi:10.3762/bjnano.13.98

• represent an obvious alternative to the oral forms, which have many limitations such as low bioavailability due to hepatic circulation and potential food interactions, delayed onset of action, and systemic side-effects [34][35][36]. In addition, oral or intravenous administration require the use of higher

• vascular endothelium with tight junctions hampering the permeation of active ingredients to the intraocular area. When designing non-invasive ophthalmic drug dosage forms, the main aim is to improve the bioavailability by increasing the diffusion across sclera, cornea, and conjunctiva [42]. In the case of

• ability to overcome the external barriers of the human body decreasing the effectiveness of topical formulations, and minimal invasiveness. Ocular drug administration is usually associated with many challenges; poor bioavailability is among the most important ones [188]. Specific physiological conditions

Antibacterial activity of a berberine nanoformulation

• Hue Thi Nguyen,
• Tuyet Nhung Pham,
• Anh-Tuan Le,
• Nguyen Thanh Thuy,
• Tran Quang Huy and
• Thuy Thi Thu Nguyen

Beilstein J. Nanotechnol. 2022, 13, 641–652, doi:10.3762/bjnano.13.56

• belongs to the class-III drugs in the biopharmaceutical classification system, indicating that BBR is a lipophilic compound that has poor absorption and low bioavailability [24]. To improve the effectiveness of BBR, many approaches have been proposed, including synergistic effects with other drugs [3

• delivery efficiency of BBR. This nanoformulation increased the oral relative bioavailability to approximately 343% compared to that of the original BBR. Although nanoformulations have emerged as an effective approach to improve the bioavailability of BBR, several drawbacks should be addressed as follows

Ciprofloxacin-loaded dissolving polymeric microneedles as a potential therapeutic for the treatment of S. aureus skin infections

• Sharif Abdelghany,
• Walhan Alshaer,
• Yazan Al Thaher,
• Maram Al Fawares,
• Amal G. Al-Bakri,
• Saja Zuriekat and
• Randa SH. Mansour

Beilstein J. Nanotechnol. 2022, 13, 517–527, doi:10.3762/bjnano.13.43

• low bioavailability of orally administered drugs due to poor absorption and enzymatic degradation in the gastrointestinal tract [3][4]. Among the different types of microneedles, dissolving microneedles have attracted research due to their advantages, which include low cost and simple preparation

Ethosomal (−)-epigallocatechin-3-gallate as a novel approach to enhance antioxidant, anti-collagenase and anti-elastase effects

• Çiğdem Yücel,
• Gökçe Şeker Karatoprak,
• Sena Yalçıntaş and
• Tuğba Eren Böncü

Beilstein J. Nanotechnol. 2022, 13, 491–502, doi:10.3762/bjnano.13.41

• neurodegenerative disorders [7][8][9]. However, there are some difficulties in the formulation of EGCG such as the first pass metabolism effect, enzymatic degradation, and low bioavailability [8][10]. Skin delivery, besides being painless and noninvasive, has many advantages such as controlled drug delivery

Micro- and nanotechnology in biomedical engineering for cartilage tissue regeneration in osteoarthritis

• Zahra Nabizadeh,
• Mahmoud Nasrollahzadeh,
• Hamed Daemi,
• Mohamadreza Baghaban Eslaminejad,
• Ali Akbar Shabani,
• Mehdi Dadashpour,
• Majid Mirmohammadkhani and
• Davood Nasrabadi

Beilstein J. Nanotechnol. 2022, 13, 363–389, doi:10.3762/bjnano.13.31

• -loaded NPs. The results of this study showed that the encapsulation of SM in PLGA NPs enhanced its chondroprotective effects by improving the stability and bioavailability of the SM [68]. Curcuminoid-loaded HA-chitosan NPs (HA-CNPs) have demonstrated excellent potential in OA treatment due to providing

Coordination-assembled myricetin nanoarchitectonics for sustainably scavenging free radicals

• Xiaoyan Ma,
• Haoning Gong,
• Kenji Ogino,
• Xuehai Yan and
• Ruirui Xing

Beilstein J. Nanotechnol. 2022, 13, 284–291, doi:10.3762/bjnano.13.23

• signal pathways and, thus, of sustainably scavenging radicals. However, Myr is poorly soluble in water, which limits its bioavailability for biomedical applications, and even its clinical therapeutic potential. The antioxidant peptide glutathione (GSH) plays a role as antioxidant in cells and possesses

• offers a new design to harness stable, sustainable antioxidant nanoparticles with high loading capacity, high bioavailability, and good biocompatibility as antioxidants. Keywords: antioxidant; co-assembly; glutathione; myricetin; nanoarchitectonics; Introduction Oxidative stress, caused by an imbalance

• phosphopeptides, exhibited huge therapeutic potential in antioxidant treatments [11][12][13]. Nevertheless, a plenty of disadvantages restrict biomedical applications, namely low biocompatibility of the metal-based nanomaterials, low bioavailability of hydrophobic small-molecule compounds, and easy degradation of

Engineered titania nanomaterials in advanced clinical applications

• Padmavati Sahare,
• Paulina Govea Alvarez,
• Juan Manual Sanchez Yanez,
• Gabriel Luna-Bárcenas,
• Samik Chakraborty,
• Sujay Paul and
• Miriam Estevez

Beilstein J. Nanotechnol. 2022, 13, 201–218, doi:10.3762/bjnano.13.15

• dendrimer nps as well as inorganic nanoscale drug carriers are currently used for drug delivery [101]. Almost all of them show higher bioavailability as their uptake mechanism is by absorptive endocytosis, and the slow release of drugs in the blood circulatory system efficiently maintains the level of

Biocompatibility and cytotoxicity in vitro of surface-functionalized drug-loaded spinel ferrite nanoparticles

• Sadaf Mushtaq,
• Khuram Shahzad,
• Tariq Saeed,
• Anwar Ul-Hamid,
• Bilal Haider Abbasi,
• Nafees Ahmad,
• Waqas Khalid,
• Muhammad Atif,
• Zulqurnain Ali and
• Rashda Abbasi

Beilstein J. Nanotechnol. 2021, 12, 1339–1364, doi:10.3762/bjnano.12.99

• bioavailability of the encapsulated drug which allows controlled release. Additionally, the attached drug is protected from degradation, which allows an increased circulation time [6]. The targeting of specific tumor tissue is therefore achieved by an increased biodistribution process known as enhanced

• potential values is the interaction between NPs and serum proteins present in DMEM [30]. In cell culture media, NPs agglomerate with serum proteins and are therefore recruited in cells via the protein corona effect, which increases the bioavailability of NPs by many folds [31]. PMA-coated samples have a

• controls. The efficient retention of polymer-functionalized NPs in cancer cells, with the help of the EPR effect and a leaky vasculature system (pore diameter = 100 nm–2 µm) [7], reduces their nonspecific biological interactions with plasma proteins, contributing to a higher bioavailability [37]. SRB

Self-assembly of amino acids toward functional biomaterials

• Huan Ren,
• Lifang Wu,
• Lina Tan,
• Yanni Bao,
• Yuchen Ma,
• Yong Jin and
• Qianli Zou

Beilstein J. Nanotechnol. 2021, 12, 1140–1150, doi:10.3762/bjnano.12.85

• promising natural antitumor drug, which can inhibit the transformation, proliferation, and migration of tumor cells through various ways, and has anti-angiogenic activity and good biocompatibility [72]. However, the poor water solubility and low bioavailability of curcumin hinder its direct application [73

• ]. Therefore, it is necessary to develop an encapsulation system to improve the bioavailability of curcumin in the tumor microenvironment in order to achieve effective delivery of curcumin and improve the therapeutic effect [74]. Li et al. [75] dissolved 9-Fmoc-ʟ-histidine (Fmoc-H) in hexafluoropropofol or

• inherent disadvantages of PS, such as hydrophobicity and easy aggregation under physiological conditions, reduce its therapeutic efficiency [77]. Using nanotechnology to encapsulate PS in nanoparticles can effectively solve this problem, improve the bioavailability of PS, and achieve targeted delivery of

Use of nanosystems to improve the anticancer effects of curcumin

• Andrea M. Araya-Sibaja,
• Norma J. Salazar-López,
• Krissia Wilhelm Romero,
• José R. Vega-Baudrit,
• J. Abraham Domínguez-Avila,
• Carlos A. Velázquez Contreras,
• Ramón E. Robles-Zepeda,
• Mirtha Navarro-Hoyos and
• Gustavo A. González-Aguilar

Beilstein J. Nanotechnol. 2021, 12, 1047–1062, doi:10.3762/bjnano.12.78

• metabolism, low bioavailability, and fast elimination of the molecule. Considering this, the present work reviews the use of CUR-based nanosystems as anticancer agents, including conventional nanosystems (i.e., liposomes, nanoemulsions, nanocrystals, nanosuspensions, polymeric nanoparticles) and nanosystems

• solubility, lack of specificity, high toxicity, poor therapy index, and multidrug resistance are other related drawbacks [6][7]. Orally administered chemotherapy is currently unsuitable due to the low bioavailability of chemotherapeutic agents [8], making intravenous the only viable route of administration

• , since it avoids bioavailability issues. However, this results in increased toxicity and side effects [3]. Therefore, one of the goals of new and/or improved cancer therapies is for the drug to only target malignant cells in sufficient concentrations and with minimal distribution to other tissues to

Comprehensive review on ultrasound-responsive theranostic nanomaterials: mechanisms, structures and medical applications

• Sepand Tehrani Fateh,
• Lida Moradi,
• Elmira Kohan,
• Michael R. Hamblin and
• Amin Shiralizadeh Dezfuli

Beilstein J. Nanotechnol. 2021, 12, 808–862, doi:10.3762/bjnano.12.64

The impact of molecular tumor profiling on the design strategies for targeting myeloid leukemia and EGFR/CD44-positive solid tumors

• Nikola Geskovski,
• Nadica Matevska-Geshkovska,
• Simona Dimchevska Sazdovska,
• Marija Glavas Dodov,
• Kristina Mladenovska and
• Katerina Goracinova

Beilstein J. Nanotechnol. 2021, 12, 375–401, doi:10.3762/bjnano.12.31

• transcription factors, but also as roadmaps for active targeting using novel nanoparticles (NPs). Furthermore, the use of nanotechnology for the delivery of cytotoxic drugs can also be valuable in facilitating cell-specific administration of drugs, improving their bioavailability, reducing side effects, and

Doxorubicin-loaded gold nanorods: a multifunctional chemo-photothermal nanoplatform for cancer management

• Uzma Azeem Awan,
• Abida Raza,
• Shaukat Ali,
• Rida Fatima Saeed and
• Nosheen Akhtar

Beilstein J. Nanotechnol. 2021, 12, 295–303, doi:10.3762/bjnano.12.24

• limited due to several unwanted characteristics of poor solubility, broad bioavailability range, narrow therapeutic index, rapid elimination from systemic circulation, unselective site of action after oral/intravenous administration, and cytotoxic effects on normal tissues [6]. The anticancer drug

Characterization, bio-uptake and toxicity of polymer-coated silver nanoparticles and their interaction with human peripheral blood mononuclear cells

• Sahar Pourhoseini,
• Reilly T. Enos,
• Angela E. Murphy,
• Bo Cai and
• Jamie R. Lead

Beilstein J. Nanotechnol. 2021, 12, 282–294, doi:10.3762/bjnano.12.23

• anti-inflammatory cytokines. Despite the increased usage of and the likely increased exposure to AgNPs, there is a lack of quantitative analysis of bio-uptake and potential cytotoxicity in PBMCs after exposure to well-characterized AgNPs. A number of studies have investigated the bioavailability and

Differences in surface chemistry of iron oxide nanoparticles result in different routes of internalization

• Barbora Svitkova,
• Vlasta Zavisova,
• Veronika Nemethova,
• Martina Koneracka,
• Miroslava Kretova,
• Filip Razga,
• Monika Ursinyova and
• Alena Gabelova

Beilstein J. Nanotechnol. 2021, 12, 270–281, doi:10.3762/bjnano.12.22

• 40–50 nm in diameter [14], or glycosylphosphatidylinositol (GPI)-anchored proteins [15]. Inorganic nanoparticles are frequently engineered with an organic surface coating to improve their biocompatibility, colloidal stability, and bioavailability. Moreover, the coating facilitates their further

PEG/PEI-functionalized single-walled carbon nanotubes as delivery carriers for doxorubicin: synthesis, characterization, and in vitro evaluation

• Shuoye Yang,
• Zhenwei Wang,
• Yahong Ping,
• Yuying Miao,
• Yongmei Xiao,
• Lingbo Qu,
• Lu Zhang,
• Yuansen Hu and
• Jinshui Wang

Beilstein J. Nanotechnol. 2020, 11, 1728–1741, doi:10.3762/bjnano.11.155

• , including CNTs [25]. Premature removal by the RES will inevitably hamper the absorption efficiency, resulting in a decrease of circulating half-life and reduced bioavailability at the intended delivery site [26][27]. Several strategies have been developed to modify particle surfaces to address this

Antimicrobial metal-based nanoparticles: a review on their synthesis, types and antimicrobial action

• Matías Guerrero Correa,
• Fernanda B. Martínez,
• Cristian Patiño Vidal,
• Camilo Streitt,
• Juan Escrig and
• Carol Lopez de Dicastillo

Beilstein J. Nanotechnol. 2020, 11, 1450–1469, doi:10.3762/bjnano.11.129

• Cu NPs. The bioavailability of these antimicrobial NPs had lower MIC values against E. coli and B. subtilis than copper hydroxide particles in suspension [143]. Silver carbon complexes with different formulations, including micelles and NPs, have also shown an antimicrobial effect since they inhibit

Key for crossing the BBB with nanoparticles: the rational design

• Sonia M. Lombardo,
• Marc Schneider,
• Akif E. Türeli and
• Nazende Günday Türeli

Beilstein J. Nanotechnol. 2020, 11, 866–883, doi:10.3762/bjnano.11.72

• study by Dal Magro et al., the brain bioavailability in mice of SLNs functionalized with an ApoE-derived peptide was studied depending on the administration route of the nanoparticles. The nanoparticles were administered either by the intraperitoneal, the intravenous or the intratracheal route [66

Luminescent gold nanoclusters for bioimaging applications

• Nonappa

Beilstein J. Nanotechnol. 2020, 11, 533–546, doi:10.3762/bjnano.11.42

• , semiconductor quantum dots suffer from toxicity and are susceptible to oxidation. In this context, atomically precise gold nanoclusters protected by thiol monolayers have emerged as a new class of luminescent nanomaterials. Low toxicity, bioavailability, photostability as well as tunable size, composition, and

• bioavailability and luminescence and were non-toxic. The AuNCFs frameworks, because of their highly luminescent nature, also allowed for better imaging compared to [Au25(SG)18]-treated cells. In vivo bioimaging Conpared to cell-line and isolated in vitro studies, in vivo imaging using animal models faces

• selective formation and imaging (Figure 8). Conclusion The unique chemical, optical and catalytic properties of gold nanoclusters have led to rapid progress in their application. This can be attributed to tunable photoluminescence, low toxicity, high bioavailability and renal clearance. The studies on

Design of a nanostructured mucoadhesive system containing curcumin for buccal application: from physicochemical to biological aspects

• Sabrina Barbosa de Souza Ferreira,
• Gustavo Braga,
• Évelin Lemos Oliveira,
• Jéssica Bassi da Silva,
• Hélen Cássia Rosseto,
• Lidiane Vizioli de Castro Hoshino,
• Mauro Luciano Baesso,
• Wilker Caetano,
• Craig Murdoch,
• Helen Elizabeth Colley and
• Marcos Luciano Bruschi

Beilstein J. Nanotechnol. 2019, 10, 2304–2328, doi:10.3762/bjnano.10.222

• due to some important characteristics. They can provide intimate contact between the dosage form and tissue, which could guarantee high drug flux through the absorbing tissue to subsequently increase drug permeation and bioavailability [14][15]. In addition, the incorporation of thermoresponsive

• formation of phenylate anions and high production of CUR radicals, since this polyphenol has demonstrated high lipophilicity (log P 3.29) and low solubility in aqueous solutions and under alkaline conditions (pH > 7) [30][31][42]. These physicochemical characteristics hinder the bioavailability and

• the cancer lesions with higher bioavailability [73]. The calculation of mucoadhesive force and adhesion work has already been discussed by other authors [70] since mucoadhesive force is the most commonly used parameter to describe mucoadhesion. However, adhesion work seems to be influenced by the

Microfluidics as tool to prepare size-tunable PLGA nanoparticles with high curcumin encapsulation for efficient mucus penetration

• Nashrawan Lababidi,
• Valentin Sigal,
• Aljoscha Koenneke,
• Konrad Schwarzkopf,
• Andreas Manz and
• Marc Schneider

Beilstein J. Nanotechnol. 2019, 10, 2280–2293, doi:10.3762/bjnano.10.220

• improved solubility and bioavailability [25]. As penetrating particulate systems also raise the question of toxicity, biocompatible systems such as poly(lactide-co-glycolide) (PLGA) (a very benign material) are considered to be well-suited. PLGA NPs have been extensively studied in the pharmaceutical field

Targeted therapeutic effect against the breast cancer cell line MCF-7 with a CuFe₂O₄/silica/cisplatin nanocomposite formulation

• B. Rabindran Jermy,
• Vijaya Ravinayagam,
• Widyan A. Alamoudi,
• Dana Almohazey,
• Hatim Dafalla,
• Lina Hussain Allehaibi,
• Abdulhadi Baykal,
• Muhammet S. Toprak and
• Thirunavukkarasu Somanathan

Beilstein J. Nanotechnol. 2019, 10, 2217–2228, doi:10.3762/bjnano.10.214

• expected health crisis [1]. However, the single modal drug delivery system is hampered by low bioavailability (about 5–10%), burst release, and lower target efficiency. Multifunctional theranostic nanoparticles that can respond to an external magnetic field for drug release and assist in bioimaging

BergaCare SmartLipids: commercial lipophilic active concentrates for improved performance of dermal products

• Florence Olechowski,
• Rainer H. Müller and
• Sung Min Pyo

Beilstein J. Nanotechnol. 2019, 10, 2152–2162, doi:10.3762/bjnano.10.208

• agents, e.g., retinol as a classical example; restoration of the natural skin barrier (recently in focus in the framework of “anti-pollution” strategies); penetration enhancement and increased bioavailability allowing for a reduced application frequency, enabling the use of active agents that could not

• primarily for the higher priced cosmetic sector. Increased penetration and bioavailability Occlusion increases the dermal penetration of many active agents. Occlusion leads to increased moisture content of the skin as well as increased percutaneous absorption of most active agents [29][30]. A simple but

• for such problematic, poorly soluble active agents such as curcumin. This increased bioavailability in the skin enables real skin effects. This study based on curcumin fluorescence was a qualitative study as the fluourescence intensity was not measured quantitatively. However, strong fluorescence

Porous silver-coated pNIPAM-co-AAc hydrogel nanocapsules

• William W. Bryan,
• Riddhiman Medhi,
• Maria D. Marquez,
• Supparesk Rittikulsittichai,
• Michael Tran and
• T. Randall Lee

Beilstein J. Nanotechnol. 2019, 10, 1973–1982, doi:10.3762/bjnano.10.194

• advantages over bulk materials in terms of reactive surface area, mobility, carrier capacity, bioavailability, and absorption/scattering across a broad range of wavelengths, even into the near-infrared (NIR) [7][8][9][10]. Nanostructured composites have been reported in a variety of shapes, sizes, and

Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells

• Liang Xu,
• Dekang Xu,
• Ziying Li,
• Yu Gao and
• Haijun Chen

Beilstein J. Nanotechnol. 2019, 10, 1933–1942, doi:10.3762/bjnano.10.189

• by cholesterol have been substantially investigated as drug carriers for targeting, modulating drug pharmacokinetics, and decreasing drug toxicity [15][16]. Liposomes also can be used as solubilizing media to enhance solubility and bioavailability of insoluble drugs [17]. Di and our prepared

• phytosomes were expected to enhance the solubility and bioavailability of the Di derivative for clinical transformation. In this study, we first prepared several Di derivatives and screened the most potent candidate through a preliminary structure–activity relationship study. Then the liposome-like