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International Journal of Molecular... Feb 2022Local drug delivery is an effective strategy for achieving direct and instant therapeutic effects. Current clinical treatments have fallen short and are limited by... (Review)
Review
Local drug delivery is an effective strategy for achieving direct and instant therapeutic effects. Current clinical treatments have fallen short and are limited by traditional technologies. Bioadhesive nanoparticles (NPs), however, may be a promising carrier for optimized local drug delivery, offering prolonged drug retention time and steadily maintained therapeutic concentrations. In addition, the possibility of clinical applications of this platform are abundant, as most polymers used for bioadhesion are both biodegradable and biocompatible. This review highlights the major advances in the investigations of polymer-based bioadhesive nanoparticles and their innumerable applications in local drug delivery.
Topics: Adhesives; Animals; Drug Carriers; Drug Delivery Systems; Excipients; Humans; Nanoparticles; Polymers
PubMed: 35216484
DOI: 10.3390/ijms23042370 -
European Journal of Pharmaceutical... May 2022Drug administration by inhalation is a well-established approach to treat respiratory and systemic diseases. To deliver a drug into the lung dry powder inhalation (DPI)... (Review)
Review
Drug administration by inhalation is a well-established approach to treat respiratory and systemic diseases. To deliver a drug into the lung dry powder inhalation (DPI) is an advantageous, but yet challenging option. A variety of strategies is available for developing DPI formulations. These formulation strategies should address the present disadvantage of insufficient drug delivery and enable therapies in general or to reach new targets (e.g. mucosal vaccination). To increase therapy safety and efficacy scientists challenge the limits of technical feasibility to engineer respiratory medicines. In this review, we provide a concise overview of particle engineering as enabling formulation technique or as an optimisation approach for existing strategies in pulmonary drug delivery. It comprehensively describes different techniques for particle engineering in carrier-based blends for inhalation. This covers considerations on which attributes are beneficial for carriers, followed by methods to modify such attributes or directly manufacture the desired carriers. Furthermore, this work comprises the current state of knowledge on nanocrystal and nanoparticle production as well as other carrier-free technologies and their applications. This review is completed by a glance in the future of carrier engineering using additive manufacturing.
Topics: Administration, Inhalation; Aerosols; Drug Delivery Systems; Dry Powder Inhalers; Excipients; Lung; Particle Size; Powders
PubMed: 35248734
DOI: 10.1016/j.ejps.2022.106158 -
European Journal of Dermatology : EJD Sep 2022Generic drugs may differ from brand-name drugs in nature and quantity of excipients. Hypersensitivity to generic drugs is a subject of growing importance given their key... (Review)
Review
Generic drugs may differ from brand-name drugs in nature and quantity of excipients. Hypersensitivity to generic drugs is a subject of growing importance given their key role in healthcare spending policies, however, a review of published data highlighted that relevant data is sparse. No scientific rationale has emerged for labelling patients allergic to all generic drugs, and hypersensitivity to generic drugs may rather be explored on a case-by-case basis. In the case of hypersensitivity without any change in medication, it is advisable to check for a switch from a brand-name to a generic drug, and if hypersensitivity to a generic drug is suspected, its composition must be checked.
Topics: Humans; Drugs, Generic; Hypersensitivity; Excipients; Product Labeling
PubMed: 36468717
DOI: 10.1684/ejd.2022.4291 -
The Journal of Allergy and Clinical... Aug 2023This guidance updates 2021 GRADE (Grading of Recommendations Assessment, Development and Evaluation) recommendations regarding immediate allergic reactions following... (Review)
Review
Updated guidance regarding the risk of allergic reactions to COVID-19 vaccines and recommended evaluation and management: A GRADE assessment and international consensus approach.
This guidance updates 2021 GRADE (Grading of Recommendations Assessment, Development and Evaluation) recommendations regarding immediate allergic reactions following coronavirus disease 2019 (COVID-19) vaccines and addresses revaccinating individuals with first-dose allergic reactions and allergy testing to determine revaccination outcomes. Recent meta-analyses assessed the incidence of severe allergic reactions to initial COVID-19 vaccination, risk of mRNA-COVID-19 revaccination after an initial reaction, and diagnostic accuracy of COVID-19 vaccine and vaccine excipient testing in predicting reactions. GRADE methods informed rating the certainty of evidence and strength of recommendations. A modified Delphi panel consisting of experts in allergy, anaphylaxis, vaccinology, infectious diseases, emergency medicine, and primary care from Australia, Canada, Europe, Japan, South Africa, the United Kingdom, and the United States formed the recommendations. We recommend vaccination for persons without COVID-19 vaccine excipient allergy and revaccination after a prior immediate allergic reaction. We suggest against >15-minute postvaccination observation. We recommend against mRNA vaccine or excipient skin testing to predict outcomes. We suggest revaccination of persons with an immediate allergic reaction to the mRNA vaccine or excipients be performed by a person with vaccine allergy expertise in a properly equipped setting. We suggest against premedication, split-dosing, or special precautions because of a comorbid allergic history.
Topics: Humans; COVID-19 Vaccines; GRADE Approach; Consensus; Vaccine Excipients; COVID-19; Hypersensitivity, Immediate; Anaphylaxis; Excipients
PubMed: 37295474
DOI: 10.1016/j.jaci.2023.05.019 -
The AAPS Journal Jan 2022The objective of this review article is to summarize literature data pertinent to potential excipient effects on intestinal drug permeability and transit. Despite the... (Review)
Review
The objective of this review article is to summarize literature data pertinent to potential excipient effects on intestinal drug permeability and transit. Despite the use of excipients in drug products for decades, considerable research efforts have been directed towards evaluating their potential effects on drug bioavailability. Potential excipient concerns stem from drug formulation changes (e.g., scale-up and post-approval changes, development of a new generic product). Regulatory agencies have established in vivo bioequivalence standards and, as a result, may waive the in vivo requirement, known as a biowaiver, for some oral products. Biowaiver acceptance criteria are based on the in vitro characterization of the drug substance and drug product using the Biopharmaceutics Classification System (BCS). Various regulatory guidance documents have been issued regarding BCS-based biowaivers, such that the current FDA guidance is more restrictive than prior guidance, specifically about excipient risk. In particular, sugar alcohols have been identified as potential absorption-modifying excipients. These biowaivers and excipient risks are discussed here. Graphical Abstract.
Topics: Animals; Biological Availability; Biopharmaceutics; Drug Compounding; Drug Development; Drug and Narcotic Control; Excipients; Humans; Permeability; Pharmaceutical Preparations; Therapeutic Equivalency
PubMed: 34988701
DOI: 10.1208/s12248-021-00670-1 -
Journal of Food and Drug Analysis Jun 2021Quality control (QC) is the most important key issue in the pharmaceutical industry to ensure the quality of drug products. Many analytical instruments and techniques in... (Review)
Review
Quality control (QC) is the most important key issue in the pharmaceutical industry to ensure the quality of drug products. Many analytical instruments and techniques in pharmaceutical analysis are applied to assess the quality and quantity of the drugs. In the current and future trends, a combination of digitization, automation and hyphenation with high throughput on-line performance will be the topics for the future of pharmaceutical QC. The hyphenated analytical techniques have recently received great attention as unique means to solve complex analytical problems in a short period of time. This review article is an update on the recent potential applications of hyphenated technique developed from the coupling of a rapid separation or induction technique (differential scanning calorimetry; DSC) and an on-line spectroscopic (Fourier transform infrared; FTIR) detection technology to carry out an one-step solid-state analysis in pharmaceutical formulation developments, including (1) intramolecular condensation of pharmaceutical polymers, (2) intramolecular cyclization of drugs and sweetener, (3) polymorphic transformation of drugs and excipients, (4) drug-polymer (excipient) interaction, (5) fast cocrystal screening and formation. This simultaneous DSC-FTIR microspectroscopy can also provide an easy and direct method for one-step screening and qualitative detection of drug stability in real time.
Topics: Calorimetry, Differential Scanning; Drug Stability; Excipients; Spectroscopy, Fourier Transform Infrared
PubMed: 35696204
DOI: 10.38212/2224-6614.3345 -
Biomolecules Nov 2019Cyclodextrins, since their discovery in the late 19th century, were mainly regarded as excipients. Nevertheless, developments in cyclodextrin research have shown that... (Review)
Review
Cyclodextrins, since their discovery in the late 19th century, were mainly regarded as excipients. Nevertheless, developments in cyclodextrin research have shown that some of these hosts can capture and include biomolecules, highlighting fatty acids and cholesterol, which implies that they are not inert and that their action may be used in specific medicinal purposes. The present review, centered on literature reports from the year 2000 until the present day, presents a comprehensive description of the known biological activities of cyclodextrins and their implications for medicinal applications. The paper is divided into two main sections, one devoted to the properties and applications of cyclodextrins as active pharmaceutical ingredients in a variety of pathologies, from infectious ailments to cardiovascular dysfunctions and metabolic diseases. The second section is dedicated to the use of cyclodextrins in a range of biomedical technologies.
Topics: Animals; Biomedical Technology; Cyclodextrins; Excipients; Humans
PubMed: 31795222
DOI: 10.3390/biom9120801 -
International Journal of Pharmaceutics Feb 2023The surface of particles is the hotspot of interaction with their environment and is therefore a major target for particle engineering. Particles with tailored coatings...
The surface of particles is the hotspot of interaction with their environment and is therefore a major target for particle engineering. Particles with tailored coatings are greatly desired for a range of different applications. Amorphous coatings applied via film coating or microencapsulation have frequently been described in the pharmaceutical context and usually result in homogeneous surfaces. In the present study we have been exploring the feasibility of coating core particles with crystalline substances, a matter that has rarely been investigated. The expansion of the range of possible coating materials to include small organic molecules enables completely new product properties to be achieved. We present an approach based on temperature cycles performed in a tubular crystallizer to result in engineered crystalline coatings on excipient core particles. By manipulating the process settings and by the choice of coating substance we are able to tailor surface roughness, topography as well as surface chemistry. Benefits of our approach are demonstrated by using resulting particles as carriers in dry-powder-inhaler formulations. Depending on the resulting surface chemistry and surface roughness, coated carrier particles show varying fitness for delivering the model API salbutamol sulphate to the lung.
Topics: Drug Carriers; Temperature; Particle Size; Powders; Administration, Inhalation; Albuterol; Dry Powder Inhalers; Excipients; Surface Properties
PubMed: 36596318
DOI: 10.1016/j.ijpharm.2022.122577 -
European Journal of Pharmaceutical... Mar 2023Non-compliance, dosing inaccuracy, choking risk, flavour, and instability, are some of the issues associated with paediatric, oral dosage forms - tablets, capsules,... (Review)
Review
Non-compliance, dosing inaccuracy, choking risk, flavour, and instability, are some of the issues associated with paediatric, oral dosage forms - tablets, capsules, solutions, and suspensions. Orally disintegrating drug carriers, a dosage form with growing interest, are thought to overcome several of the challenges associated with these conventional formulations by rapidly disintegrating within the buccal cavity without the need for water. This review serves as an up-to-date report on the various types of orodispersible delivery systems, currently being developed or commercialized, by detailing their characteristics, manufacturing processes, and applications in the paediatric population. Mentioned are orodispersible tablets, films, wafers and lyophilisates, mini-tablets, capsules, granules, electrospun fibers and webs. Also highlighted are the choice of excipients, quality control requirements, and expected pharmacokinetics of orally disintegrating drug carriers concerning the paediatric population. Overall, orodispersible formulations, particularly tablets, films, and lyophilisates/wafers, have shown to be a valuable addition to medication administration in minors, thus the execution of more targeted research and development activities is expected to lead to enhanced paediatric care and outcomes.
Topics: Humans; Child; Drug Carriers; Administration, Oral; Tablets; Drug Compounding; Excipients; Solubility
PubMed: 36634740
DOI: 10.1016/j.ejps.2023.106377 -
Carbohydrate Polymers Jun 2024Sodium Sulfobutylether-β-cyclodextrin (SBE-β-CD) is a derivative of β-cyclodextrin, characterized by its stereo structure, which closely resembles a truncated cone... (Review)
Review
Sodium Sulfobutylether-β-cyclodextrin (SBE-β-CD) is a derivative of β-cyclodextrin, characterized by its stereo structure, which closely resembles a truncated cone with a hydrophobic internal cavity. The solubility of insoluble substances within the hydrophobic cavity is significantly enhanced, reducing contact between the guest and the environment. Consequently, SBE-β-CD is frequently employed as a co-solvent and stabilizer. As the research progresses, it has been observed that the inclusion of SBE-β-CD is reversible and competitive. Besides, some inclusion complexes undergo distinct physicochemical property alterations compared to the guests. Additionally, certain guests exhibit varying inclusions with SBE-β-CD at different concentrations. These features have contributed to the expanding applications. SBE-β-CD finds widespread application in pharmaceutics as a protective agent and pK regulator, in pharmaceutical analysis as a chiral substance separator, and in biomedical engineering for encapsulating dyes and modifying sensors. The article will elaborate in detail on the physicochemical properties of SBE-β-CD, encapsulation principles, and factors influencing the formation of inclusion complexes. Furthermore, the review focuses on the application of SBE-β-CD through encapsulation in pharmaceutics, pharmaceutical analysis, and biomedical engineering. Finally, the prospects and potential applications of SBE-β-CD are discussed.
Topics: beta-Cyclodextrins; Excipients; Solubility; Cyclodextrins
PubMed: 38494236
DOI: 10.1016/j.carbpol.2024.121985