A Nanocrystals-Based Topical Drug Delivery System with Improved Dermal Penetration and Enhanced Treatment of Skin Diseases

2021 ◽  
Vol 17 (12) ◽  
pp. 2319-2337
Author(s):  
Lin Sun ◽  
Hong Xiang ◽  
Canfeng Ge ◽  
Xingxu Chen ◽  
Qian Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Skin Disease ◽  
Skin Diseases ◽  
Drug Loading ◽  
Clinical Trial Data ◽  
Topical Delivery ◽  
Active Pharmaceutical Ingredient ◽  
Topical Drug Delivery ◽  
Sustained Drug Release ◽  
Drug Nanocrystal

Topical drug delivery methods are important in the treatment of skin diseases. Drug nanocrystals, which are nanometersized particles of active pharmaceutical ingredients, offer efficient topical delivery with high stability, high drug loading capacity, steady dissolution, and sustained drug release profiles. The use of nanocrystals for the topical delivery of skin disease therapies is currently being evaluated; this review focuses on how nanocrystals facilitate active pharmaceutical ingredient transport across skin barriers, exploring the underlying transportation mechanisms of the nanocrystals and active pharmaceutical ingredient molecules to the dermal and epidermal skin cells. In topical delivery, previous skin treatments, choice of excipients and vehicles, and penetration enhancement strategies critically influence the topical delivery of drug nanocrystals. Various research and applications of drug nanocrystals in skin disease therapy are highlighted in this review, and intellectual property protection for drug nanocrystal formulations, clinical trial data, and products with commercial potential are also discussed.

scholarly journals Nanotechnology for Topical Drug Delivery to the Anterior Segment of the Eye

2021 ◽  
Vol 22 (22) ◽  
pp. 12368
Author(s):  
Alexander Vaneev ◽  
Victoria Tikhomirova ◽  
Natalia Chesnokova ◽  
Ekaterina Popova ◽  
Olga Beznos ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Anterior Segment ◽  
Drug Carriers ◽  
Ocular Tissue ◽  
Eye Drops ◽  
Topical Drug Delivery ◽  
Natural Polymers ◽  
Drug Bioavailability ◽  
Sustained Drug Release

Topical drug delivery is one of the most challenging aspects of eye therapy. Eye drops are the most prevalent drug form, especially for widely distributed anterior segment eye diseases (cataracts, glaucoma, dry eye syndrome, inflammatory diseases, etc.), because they are convenient and easy to apply by patients. However, conventional drug formulations are usually characterized by short retention time in the tear film, insufficient contact with epithelium, fast elimination, and difficulties in overcoming ocular tissue barriers. Not more than 5% of the total drug dose administered in eye drops reaches the interior ocular tissues. To overcome the ocular drug delivery barriers and improve drug bioavailability, various conventional and novel drug delivery systems have been developed. Among these, nanosize carriers are the most attractive. The review is focused on the different drug carriers, such as synthetic and natural polymers, as well as inorganic carriers, with special attention to nanoparticles and nanomicelles. Studies in vitro and in vivo have demonstrated that new formulations could help to improve the bioavailability of the drugs, provide sustained drug release, enhance and prolong their therapeutic action. Promising results were obtained with drug-loaded nanoparticles included in in situ gel.

scholarly journals Miktoarm Star Polymers: Branched Architectures in Drug Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 827 ◽  
Author(s):  
Victor Lotocki ◽  
Ashok Kakkar
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Therapeutic Interventions ◽  
Structure Property ◽  
Sustained Drug Release ◽  
Amphiphilic Macromolecules ◽  
Miktoarm Star ◽  
Core Junction

Delivering active pharmaceutical agents to disease sites using soft polymeric nanoparticles continues to be a topical area of research. It is becoming increasingly evident that the composition of amphiphilic macromolecules plays a significant role in developing efficient nanoformulations. Branched architectures with asymmetric polymeric arms emanating from a central core junction have provided a pivotal venue to tailor their key parameters. The build-up of miktoarm stars offers vast polymer arm tunability, aiding in the development of macromolecules with adjustable properties, and allows facile inclusion of endogenous stimulus-responsive entities. Miktoarm star-based micelles have been demonstrated to exhibit denser coronae, very low critical micelle concentrations, high drug loading contents, and sustained drug release profiles. With significant advances in chemical methodologies, synthetic articulation of miktoarm polymer architecture, and determination of their structure-property relationships, are now becoming streamlined. This is helping advance their implementation into formulating efficient therapeutic interventions. This review brings into focus the important discoveries in the syntheses of miktoarm stars of varied compositions, their aqueous self-assembly, and contributions their formulations are making in advancing the field of drug delivery.

Topical Drug Delivery of Anti-infectives Employing Lipid-Based Nanocarriers: Dermatokinetics as an Important Tool

2019 ◽  
Vol 24 (43) ◽  
pp. 5108-5128 ◽  
Author(s):  
Kanika Thakur ◽  
Gajanand Sharma ◽  
Bhupindar Singh ◽  
Om Prakash Katare
Keyword(s):  
Drug Delivery ◽  
Infectious Diseases ◽  
Patient Compliance ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Controlled Drug Release ◽  
Topical Drug Delivery ◽  
Promising Strategy ◽  
Drug Resistant Strains

Background:The therapeutic approaches for the management of topical infections have always been a difficult approach due to lack of efficacy of conventional topical formulations, high frequency of topical applications and non-patient compliance. The major challenge in the management of topical infections lies in antibiotic resistance which leads to severe complications and hospitalizations resulting in economic burden and high mortality rates.Methods:Topical delivery employing lipid-based carriers has been a promising strategy to overcome the challenges of poor skin permeation and retention along with large doses which need to be administered systemically. The use of lipid-based delivery systems is a promising strategy for the effective topical delivery of antibiotics and overcoming drug-resistant strains in the skin. The major systems include transfersomes, niosomes, ethosomes, solid lipid nanoparticles, nanostructured lipid carriers, microemulsion and nanoemulsion as the most promising drug delivery approaches to treat infectious disorders. The main advantages of these systems include lipid bilayer structure which mimics the cell membrane and can fuse with infectious microbes. The numerous advantages associated with nanocarriers like enhanced efficacy, improvement in bioavailability, controlled drug release and ability to target the desired infectious pathogen have made these carriers successful.Conclusion:Despite the number of strides taken in the field of topical drug delivery in infectious diseases, it still requires extensive research efforts to have a better perspective of the factors that influence drug permeation along with the mechanism of action with regard to skin penetration and deposition. The final objective of the therapy is to provide a safe and effective therapeutic approach for the management of infectious diseases affecting topical sites leading to enhanced therapeutic efficacy and patient-compliance.

scholarly journals Production of Drug Delivery Systems Using Fused Filament Fabrication: A Systematic Review

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 517 ◽  
Author(s):  
Bahaa Shaqour ◽  
Aseel Samaro ◽  
Bart Verleije ◽  
Koen Beyers ◽  
Chris Vervaet ◽  
...  
Keyword(s):  
Systematic Review ◽  
Drug Delivery ◽  
Preparation Method ◽  
Drug Loading ◽  
Active Pharmaceutical Ingredient ◽  
Healthcare Sector ◽  
Polymeric Carrier ◽  
Fused Filament Fabrication ◽  
Drug Delivery Devices ◽  
Potential Use

Fused filament fabrication (FFF) 3D printing technology is widely used in many fields. For almost a decade, medical researchers have been exploring the potential use of this technology for improving the healthcare sector. Advances in personalized medicine have been more achievable due to the applicability of producing drug delivery devices, which are explicitly designed based on patients’ needs. For the production of these devices, a filament—which is the feedstock for the FFF 3D printer—consists of a carrier polymer (or polymers) and a loaded active pharmaceutical ingredient (API). This systematic review of the literature investigates the most widely used approaches for producing drug-loaded filaments. It also focusses on several factors, such as the polymeric carrier and the drug, loading capacity and homogeneity, processing conditions, and the intended applications. This review concludes that the filament preparation method has a significant effect on both the drug homogeneity within the polymeric carrier and drug loading efficiency.

PLGA Nanoparticles for Anti Tuberculosis Drug Delivery

2012 ◽  
Vol 584 ◽  
pp. 465-469 ◽  
Author(s):  
S. Malathi ◽  
S. Balasubramanian
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Double Emulsion ◽  
Plga Nanoparticles ◽  
Release Mechanism ◽  
Sustained Drug Release ◽  
Drug Release Kinetics ◽  
Evaporation Technique

Nanoparticles-based drug delivery systems have considerable potential for the treatment of tuberculosis (TB). A series of PLGA polymers with different molar feed ratios (P2:87/13, P3:83/17, P5:63/37, P6:76/24, P9:53/47) were synthesized by direct melt poly condensation method. The resulting biodegradable polymers were characterized by FTIR and 1H NMR spectroscopy. The preparation of the drug (Pyrazinamide (PZA)) encapsulated PLGA polymers were carried out by double emulsion – solvent evaporation technique. The drug loaded PLGA-NPs were analyzed by UV-visible spectroscopy and scanning electron microscopy. The drug loading efficiency and drug release kinetics varies in the following order: P9>P5>P6>P3>P2. Among the formulations, PP9 showed a uniform as well as sustained drug release. The drug release kinetics has been evaluated by Zero-order, First order, Higuchi and Koresmeyer- Peppas models and the release mechanism has also been investigated

scholarly journals Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

2021 ◽  
Vol 22 (4) ◽  
pp. 1535
Author(s):  
Parinbhai Shah ◽  
Benjamin Goodyear ◽  
Nirali Dholaria ◽  
Vinam Puri ◽  
Bozena Michniak-Kohn
Keyword(s):  
Drug Delivery ◽  
Skin Diseases ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Oral Drug ◽  
Ionic Surfactant ◽  
Content Uniformity ◽  
Drug Bioavailability ◽  
Drug Content

Psoriasis is a chronic autoimmune skin disease impacting the population globally. Pharmaceutical products developed to combat this condition commonly used in clinical settings are IV bolus or oral drug delivery routes. There are some major challenges for effectively developing new dosage forms for topical use: API physicochemical nature, the severity of the disease state, and low bioavailability present challenges for pharmaceutical product developers. For non-severe cases of psoriasis, topical drug delivery systems may be preferred or used in conjunction with oral or parenteral therapy to address local symptoms. Elastic vesicular systems, termed “niosomes”, are promising drug delivery vehicles developed to achieve improved drug delivery into biological membranes. This study aimed to effectively incorporate a corticosteroid into the niosomes for improving the drug bioavailability of desoximetasone, used to treat skin conditions via topical delivery. Niosomes characterization measurements were drug content, pH, spreadability, specific gravity, content uniformity, rheology, and physicochemical properties. Formulations used a topical gelling agent, Carbomer 980 to test for in vitro skin permeation testing (IVPT) and accelerated stability studies. The developed niosomal test gel provided approximately 93.03 ± 0.23% to 101.84 ± 0.11% drug content with yield stresses ranging from 16.12 to 225.54 Pa. The permeated amount of desoximetasone from the niosomal gel after 24 h was 9.75 ± 0.44 µg/cm2 compared to 24.22 ± 4.29 µg/cm2 released from the reference gel tested. Furthermore, a drug retention study compared the test gel to a reference gel, demonstrating that the skin retained 30.88 ng/mg of desoximetasone while the reference product retained 26.01 ng/mg. A controlled drug release profile was obtained with a niosomal formulation containing desoximetasone for use in a topical gel formulation showing promise for potential use to treat skin diseases like psoriasis.

A novel composite scaffold comprising ultralong hydroxyapatite microtubes and chitosan: preparation and application in drug delivery

2017 ◽  
Vol 5 (21) ◽  
pp. 3898-3906 ◽  
Author(s):  
Yong-Gang Zhang ◽  
Ying-Jie Zhu ◽  
Feng Chen ◽  
Tuan-Wei Sun
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Composite Scaffold ◽  
Drug Loading ◽  
Loading Capacity ◽  
Sustained Drug Release ◽  
High Drug ◽  
High Drug Loading

The composite scaffold comprising ultralong hydroxyapatite microtubes and chitosan with high drug loading capacity and sustained drug release properties has been successfully prepared.

scholarly journals Development and Characterization of a Fucoidan-Based Drug Delivery System by Using Hydrophilic Anticancer Polysaccharides to Simultaneously Deliver Hydrophobic Anticancer Drugs

Biomolecules ◽  
2020 ◽  
Vol 10 (7) ◽  
pp. 970 ◽  
Author(s):  
Yen-Ho Lai ◽  
Chih-Sheng Chiang ◽  
Chin-Hao Hsu ◽  
Hung-Wei Cheng ◽  
San-Yuan Chen
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Anticancer Drugs ◽  
Delivery System ◽  
Drug Loading ◽  
Sulfated Polysaccharide ◽  
Plga Nanoparticles ◽  
Aqueous Environment ◽  
Sustained Drug Release ◽  
Hydrophobic Anticancer Drugs

Fucoidan, a natural sulfated polysaccharide, which can activate the immune response and lessen adverse effects, is expected to be an adjuvant agent in combination with chemotherapy. Using natural hydrophilic anticancer polysaccharides to simultaneously encapsulate hydrophobic anticancer drugs is feasible, and a reduced side effect can be achieved to amplify the therapeutic efficacy. In this study, a novel type of fucoidan-PLGA nanocarrier (FPN-DTX) was developed for the encapsulation of the hydrophobic anticancer drug, docetaxel (DTX), as a drug delivery system. From the comparison between FPN-DTX and the PLGA particles without fucoidan (PLGA-DTX), FPNs–DTX with fucoidan were highly stable with smaller sizes and dispersed well without aggregations in an aqueous environment. The drug loading and release can be further modified by modulating relative ratios of Fucoidan (Fu) to PLGA. The (FPN 3-DTX) nanoparticles with a 10:3 ratio of Fu:PLGA displayed uniform particle size with higher encapsulation efficiency than PLGA NPs and sustained drug release ability. The biocompatible fucoidan-PLGA nanoparticles displayed low cytotoxicity without drug loading after incubation with MDA-MB-231 triple-negative breast cancer cells. Despite lower cellular uptake than that of PLGA-DTX due to a higher degree of negative zeta potential and hydrophilicity, FPN 3-DTX effectively exerted better anticancer ability, so FPN 3-DTX can serve as a competent drug delivery system.

scholarly journals Non-Invasive Topical Drug-Delivery System Using Hyaluronate Nanogels Crosslinked via Click Chemistry

Materials ◽  
2021 ◽  
Vol 14 (6) ◽  
pp. 1504
Author(s):  
Hyunsik Choi ◽  
Mina Kwon ◽  
Hye Eun Choi ◽  
Sei Kwang Hahn ◽  
Ki Su Kim
Keyword(s):  
Drug Delivery ◽  
Click Chemistry ◽  
Topical Delivery ◽  
Topical Drug Delivery ◽  
Safety Issues ◽  
Non Invasive ◽  
Therapeutic Drugs ◽  
Delivery Routes ◽  
Model Drug

Hyaluronate (HA) has been widely investigated for noninvasive topical drug delivery of chemical drugs and biopharmaceuticals. However, previous noninvasive delivery systems have been facilitated mostly by chemical conjugation of drugs with HA, which can cause reduced therapeutic efficacy and safety issues in chemically modified drugs. Here, HA nanogels were synthesized by crosslinking via “click” chemistry for noninvasive topical delivery of a model drug without chemical modification. The model-drug-encapsulating HA nanogels could be uptaken to the skin melanoma cells in vitro by HA-mediated endocytosis. In addition, histological analysis showed that HA nanogels could be topically delivered to the deep skin and tongue tissues through the noninvasive delivery routes. Taken together, HA nanogels could be effectively used for the noninvasive topical delivery of various therapeutic drugs.

scholarly journals Potential advancements of nanocarriers in topical drug delivery: a mini review

2020 ◽  
Vol 9 (2) ◽  
pp. 968-974
Keyword(s):  
Drug Delivery ◽  
Targeted Drug Delivery ◽  
Molecular Mechanisms ◽  
Chemical Nature ◽  
Skin Diseases ◽  
Topical Drug Delivery ◽  
Drug Candidates ◽  
Bio Imaging ◽  
Drug Doses ◽  
Lowering Drug

The topical route offers many attractive alternatives for the drug delivery as compared to oral administration and injection. Besides, skin provides a reservoir that delivers drug delivery for days. Nanotechnology, science at nano scale, has been emerged as a strong and potential discipline focusing on atom and molecular mechanisms that contributes to a diversity of applications in various fields such as controlled and targeted drug delivery, bio-imaging, agriculture, 3D printing, physics, mechanics, etc. Nanocarriers avoid local irritation and toxicity. The nanocarrier drug delivery system has emerged as interesting field that broaden up the use various drugs (lipophillic and hydrophilic) and provides ease of fabrication of formulations that can be efficiently delivered via topical route. The nanocarrier based delivery has been explored to deliver hydrophilic and lipophilic drug candidates through stratum corneum with local and systemic effects for the treatment of variety different skin diseases. Nanocarriers such as a nanoparticle, dendrimer, ethosome, and liposome are made up of polymers and material that differ in structure and chemical nature. These nanocarriers can deliver the drug at the target site and reduce side effects by lowering drug doses. This review covers all aspects of pharmaceutical nanocarriers related to their applications and recent advancements.

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