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Assay and Drug Development Technologies Oct 2021(Review)
Review
Topics: Administration, Oral; Drug Delivery Systems; Humans; Nanoparticles; Pharmaceutical Preparations; Powders; Technology, Pharmaceutical
PubMed: 34550790
DOI: 10.1089/adt.2021.053 -
Clinical Infectious Diseases : An... Mar 1997Much early experience with antibiotic therapy involved oral administration of sulfonamides, penicillins, tetracyclines, and chloramphenicol. Newer acid-labile,... (Review)
Review
Much early experience with antibiotic therapy involved oral administration of sulfonamides, penicillins, tetracyclines, and chloramphenicol. Newer acid-labile, less-soluble agents created the need for intravenous (i.v.) administration, and i.v. technology (hyporeactive catheter polymers, infusion pumps, etc.) improved to where i.v. administration became normative for the treatment of serious infections. Recently, this preference is being reconsidered in light of agents that are highly effective orally, growing appreciation that i.v. treatment has serious complications, and economic pressures to provide the best care at the lowest cost. This article presents a brief history of administration routes and reviews the rationale for considering oral treatment for serious infections, including consideration of pharmacokinetics and minimum inhibitory concentrations. Published reports supporting the efficacy of orally administered antibiotics either as sole treatment or following an initial parenteral course are reviewed in detail, and examples of programs that educate physicians about the rationale, acceptibility, and benefits of oral administration are given.
Topics: Administration, Oral; Anti-Bacterial Agents; Humans
PubMed: 9114201
DOI: 10.1093/clinids/24.3.457 -
Drug Delivery Dec 2023Amphotericin B (AmB) is regarded as a first-line therapy against life-threatening invasive fungal infections. Due to its poor oral bioavailability, AmB is restricted to... (Review)
Review
Amphotericin B (AmB) is regarded as a first-line therapy against life-threatening invasive fungal infections. Due to its poor oral bioavailability, AmB is restricted to intravenous administration in clinical practice. As science continues to move forward, two lipid-based formulations are successfully developed for oral AmB administration, currently undergoing phase I clinical trials. Encouragingly, lipid-AmB conjugates with emulsions also exhibit a better bioavailability, which may be another strategy to design oral AmB formulation in clinical practice. Thus, this review mainly focused on the two lipid-based formulations in clinical trials, and discussed the potential perspectives of AmB-lipid conjugation-loaded nanocochleates and emulsions.
Topics: Amphotericin B; Antifungal Agents; Emulsions; Administration, Oral; Anti-Bacterial Agents; Macrolides; Lipids
PubMed: 36601799
DOI: 10.1080/10717544.2022.2161671 -
International Journal of Pharmaceutics Nov 2022This paper reviews many of the properties of a peptide that need to be considered prior to development as an oral dosage form when co-formulated with a permeation... (Review)
Review
This paper reviews many of the properties of a peptide that need to be considered prior to development as an oral dosage form when co-formulated with a permeation enhancer to improve oral bioavailability, including the importance and implications of peptide half-life on variability in pharmacokinetic profiles. Clinical considerations in terms of food and drug-drug interactions are also discussed. The paper further gives a brief overview how permeation enhancers overcome barriers that limit oral absorption of peptides and thereby improve their oral bioavailability, albeit bioavailabilities are still low single digit and variability is high.
Topics: Drug Delivery Systems; Administration, Oral; Peptides; Biological Availability; Half-Life
PubMed: 36174850
DOI: 10.1016/j.ijpharm.2022.122238 -
International Journal of Pharmaceutics Dec 2022Medical use of hydrogen gas (H) has been given increasing attention over the past 15 years with numerous clinical trials for a variety of indications. The biological...
Medical use of hydrogen gas (H) has been given increasing attention over the past 15 years with numerous clinical trials for a variety of indications. The biological activity of H includes antioxidant properties and thereby the ability to neutralize damaging reactive oxygen species (ROS). Administration of hydrogen as a medical gas is limited by the poor water solubility and by the flammability of H in air. Therefore, nanocarriers have been investigated for safer and more efficient administration of hydrogen. Silicon particles are suggested for oral administration with the ability to undergo a redox reaction with water to produce Hin vivo. The purpose of this work was to investigate the hydrogen generating abilities of silicon particles synthesized by centrifugal chemical vapor deposition (cCVD). High hydrogen generation rates up to 1310 ml/g at physiological pH 7.4 (82 % yield) were observed. An in vitro model of oral administration showed that pretreatment in artificial gastric juice did not affect hydrogen generation. Thus, the cCVD silicon particles seem to be suitable for in vivo hydrogen generation. A surface carbon coating or addition of surfactants or albumin hindered hydrogen generation. The addition of egg white reduced hydrogen generation but did not block it.
Topics: Silicon; Hydrogen; Nanoparticles; Administration, Oral; Water
PubMed: 36351504
DOI: 10.1016/j.ijpharm.2022.122371 -
Drug Development and Industrial Pharmacy May 2017
Topics: Administration, Oral; Biological Availability; Humans
PubMed: 28253737
DOI: 10.1080/03639045.2017.1290865 -
Advanced Drug Delivery Reviews Mar 2019Since the development of self-emulsifying drug delivery systems (SEDDS) in 1980's, they attract the attention of researchers in order to confront the challenge of poor... (Review)
Review
Since the development of self-emulsifying drug delivery systems (SEDDS) in 1980's, they attract the attention of researchers in order to confront the challenge of poor water-solubility of orally given drugs. Within recent years, SEDDS were also discovered for oral administration of hydrophilic macromolecular drugs such as peptides, proteins, polysaccharides and pDNA. Due to hydrophobic ion pairing (HIP) with oppositely charged lipophilic auxiliary agents the resulting complexes can be incorporated in the lipophilic phase of SEDDS. Depending on the solubility of the complex in the SEDDS pre-concentrate and in the release medium drug release can be adjusted on purpose by choosing more or less lipophilic auxiliary agents in appropriate quantities for HIP. Within the oily droplets formed in the GI-tract drugs are protected towards degradation by proteases and nucleases and thiol-disulfide exchange reactions with dietary proteins. The oily droplets can be made mucoadhesive or highly mucus permeating depending on their target site. Furthermore, even their cellular uptake properties can be tuned by adjusting their zeta potential or decorating them with cell penetrating peptides. The potential of SEDDS for oral administration of hydrophilic macromolecular drugs could meanwhile be demonstrated via various in vivo studies showing a bioavailability at least in the single digit percentage range. Owing to these properties advanced SEDDS turned out to be a game changing approach for the oral administration of hydrophilic macromolecular drugs.
Topics: Administration, Oral; Animals; Drug Delivery Systems; Emulsions; Humans; Hydrophobic and Hydrophilic Interactions; Pharmaceutical Preparations
PubMed: 29981355
DOI: 10.1016/j.addr.2018.07.001 -
American Journal of Health-system... Feb 2015Available data regarding sublingual tacrolimus were analyzed to provide recommendations for solid organ transplant recipients. (Comparative Study)
Comparative Study Meta-Analysis Review
PURPOSE
Available data regarding sublingual tacrolimus were analyzed to provide recommendations for solid organ transplant recipients.
SUMMARY
Tacrolimus is an immunosuppressive agent with a narrow therapeutic range that is commonly used in solid organ transplantation. Achieving and maintaining appropriate tacrolimus exposure are critical for preventing rejection and minimizing toxicity. A variety of clinical situations requiring nonoral medication delivery arise, presenting the need for reliable alternative routes of tacrolimus administration. A review of the currently available literature revealed nine reports of sublingual tacrolimus use in human subjects. Seven reported that sublingual administration could achieve comparable tacrolimus trough concentrations to oral administration, but none investigated the correlation between tacrolimus trough concentration and exposure. One study of lung transplant recipients found that approximately 50% of the oral dose was needed to obtain therapeutic trough concentrations when converted to sublingual administration. Another study of patients with end-stage renal disease identified a similar sublingual:oral dosing ratio of 1:2. When converted from oral tacrolimus in combination with clotrimazole to sublingual administration, the sublingual:oral dosing ratio was 1:1.
CONCLUSION
In addition to enteral tube and i.v. tacrolimus dosing, sublingual administration may be considered for short-term use in patients who are unable to receive medications orally. Based on the available data, it is reasonable to initiate sublingual tacrolimus at 50% of the current or anticipated oral dose in the absence of interacting medications. Dosing must be individualized, taking into consideration concomitant interacting medications, and adjusted to target levels based on therapeutic drug monitoring.
Topics: Administration, Oral; Administration, Sublingual; Humans; Immunosuppressive Agents; Organ Transplantation; Tacrolimus
PubMed: 25631834
DOI: 10.2146/ajhp140322 -
Pharmaceutical Patent Analyst Nov 2022Insulin, on oral administration, is very troublesome because of its limited bioavailability. The evolution of oral insulin delivery formulations is greatly desired for... (Review)
Review
Insulin, on oral administration, is very troublesome because of its limited bioavailability. The evolution of oral insulin delivery formulations is greatly desired for non-invasive therapy by overcoming its low bioavailability, GIT enzymatic deactivation, poor lipophilicity and low stability. Different approaches have been proposed to boost oral insulin bioavailability in insulin-delivery systems and emerging effective therapies by using nanoparticle formulation, nanocapsid, modified chitosan particles, polydopamine microcapsules and nanoliposomes. The present review includes patents and patent applications that were published between 2017 and January 2022.
Topics: Insulin; Drug Delivery Systems; Administration, Oral; Chitosan; Nanoparticles
PubMed: 36354044
DOI: 10.4155/ppa-2022-0017 -
Advanced Materials (Deerfield Beach,... Feb 2024Compared to injection administration, oral administration is free of discomfort, wound infection, and complications and has a higher compliance rate for patients with... (Review)
Review
Compared to injection administration, oral administration is free of discomfort, wound infection, and complications and has a higher compliance rate for patients with diverse diseases. However, oral administration reduces the bioavailability of medicines, especially biologics (e.g., peptides, proteins, and antibodies), due to harsh gastrointestinal biological barriers. In this context, the development and prosperity of nanotechnology have helped improve the bioactivity and oral availability of oral medicines. On this basis, first, the biological barriers to oral administration are discussed, and then oral nanomedicine based on organic and inorganic nanomaterials and their biomedical applications in diverse diseases are reviewed. Finally, the challenges and potential opportunities in the future development of oral nanomedicine, which may provide a vital reference for the eventual clinical transformation and standardized production of oral nanomedicine, are put forward.
Topics: Humans; Nanomedicine; Nanotechnology; Nanostructures; Pharmaceutical Preparations; Administration, Oral; Drug Delivery Systems
PubMed: 37724825
DOI: 10.1002/adma.202306081