Abstract：
:Access to medicines, including their availability and affordability, is a major public health challenge worldwide. This research aimed to characterise rectal formulations containing amoxicillin for the treatment of pneumonia in children under five, as an accessible alternative to existing formulations. Lipophilic Suppocire (S-NA15) and hydrophilic polyethylene glycol (PEG; 80% PEG 1500 and 20% PEG 4000, w/w) suppositories containing 250 mg amoxicillin were prepared. Hardness, apparent viscosity, uniformity of mass, uniformity of content, disintegration and dissolution time were determined. Irritation potential was screened using a slug mucosal assay and antibacterial efficacy against Staphylococcus aureus determined by isothermal microcalorimetry. Both lipophilic and hydrophilic formulations met the European Pharmacopoeia standards for suppositories when tested in vitro. They disintegrated within 30 min with rapid amoxicillin release profiles (98.6 ± 0.9%, 94.9 ± 1.2% over 30 min, respectively). Over-encapsulation of S-NA15 suppositories with hydroxypropyl methylcellulose shells slowed drug release and improved stability over 2 months. S-NA15 suppositories were classified as non-irritant and PEG suppositories only mildly irritant. Antibacterial efficacy of formulations was equivalent to amoxicillin alone. Both PEG and over-encapsulated S-NA15 rectal formulations developed in the present work have shown promise based on pre-clinical screening, and further development is justified to develop a product with commercial potential.
journal_name
Drug Deliv Transl Resjournal_title
Drug delivery and translational researchauthors
Hanning SM,Matiz S,Krasser K,Orlu M,Dodoo C,Gaisford S,Tuleu Cdoi
10.1007/s13346-020-00804-6subject
Has Abstractpub_date
2020-06-25 00:00:00eissn
2190-393Xissn
2190-3948pii
10.1007/s13346-020-00804-6pub_type
杂志文章abstract：:Oil in water nano-emulsions are drug delivery systems constituted by liquid lipophilic nano-droplets dispersed through the external aqueous phase, often reaching the kinetic stability with surfactant as stabilizers. Essential oils can be the oily phase or the source of bioactive compounds. In this study, the essential...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00846-w
更新日期：2020-12-01 00:00:00
abstract：:In this study, we developed, characterized, and tested in vivo polymeric nanoparticle of ethambutol labeled with 99mTc as nanoradiopharmaceutical for early diagnosis of tuberculosis by single-photon emission computed tomography, also as a therapeutic choice. Nanoparticles were developed by double emulsification. All c...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0577-6
更新日期：2019-02-01 00:00:00
abstract：:The objective of this research was to develop polymeric micellar formulations of inhibitors of signal transducer and activator of transcription 3 (STAT3) dimerization, i.e., S3I-1757 and S3I-201, and evaluate the activity of successful formulations in B16-F10 melanoma, a STAT3 hyperactive cancer model, in vitro and in...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0369-4
更新日期：2017-08-01 00:00:00
abstract：:A new PEGylated liposomal formulation containing both gemcitabine (GEM) and paclitaxel (PTX) was investigated in order to realize an innovative multidrug carrier (MDC) to test on human cancer cells. The MDC in question was realized by the liposome extrusion method. Photocorrelation spectroscopy was used for the physic...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-010-0007-x
更新日期：2011-02-01 00:00:00
abstract：:Oral pre-exposure prophylaxis for the prevention of HIV-1 transmission (HIV PrEP) has been widely successful as demonstrated by a number of clinical trials. However, studies have also demonstrated the need for patients to tightly adhere to oral dosing regimens in order to maintain protective plasma and tissue concentr...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-017-0391-6
更新日期：2017-12-01 00:00:00
abstract：:RNAi-based nanomedicine platforms (RNPs) have progressed from tools to study gene expression in vitro into clinical trials. Numerous RNPs strategies have been documented with an efficient ability to condense RNAi payloads and induce potent gene silencing. Moreover, some of these RNPs have been explored in various anim...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-013-0158-7
更新日期：2014-02-01 00:00:00
abstract：:Curcumin (CUR), a natural polyphenolic compound, is considered as one of the most potential candidates against Alzheimer disease (AD) by targeting multiple pathologies such as amyloid-beta, tau phosphorylation, and oxidative stress. Poor physicochemical profile and oral bioavailability (BA) are the major contributors ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0570-0
更新日期：2018-10-01 00:00:00
abstract：:High-energy methods for the manufacturing of nanomedicines are widely used; however, interest in low-energy methods is increasing due to their simplicity, better control over the process, and energy-saving characteristics during upscaling. Here, we developed a novel lipid-core micelle (LCM) as a nanocarrier to encapsu...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0521-9
更新日期：2018-12-01 00:00:00
abstract：:Dry powder inhalers (DPIs) have been proposed as an alternative administration route for protein and peptide drugs. However, DPI particles are easy to aggregate due to the strong interactions between the particles, leading to poor aerosolization performance. In this study, fragmented particles containing octreotide ac...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0515-7
更新日期：2018-06-01 00:00:00
abstract：:In this work, we studied the effect of gamma irradiation on nano-bioactive glass (NBG) structure, bioactivity, drug loading efficiency, and drug release kinetic. Gamma irradiation was mainly introduced as a safe and cheap method to tailor the drug loading and release efficiencies. NBG was investigated before and after...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-014-0214-y
更新日期：2015-02-01 00:00:00
abstract：:Polyelectrolyte nanoparticle constructs (NPs) comprising salmon calcitonin (sCT), chitosan (CS), and hyaluronic acid (HA) were previously established as having anti-inflammatory potential when injected via the intra-articular (i.a.) route to a mouse model. We attempted to translate the formulation to a large animal mo...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0557-x
更新日期：2018-10-01 00:00:00
abstract：:This study evaluated effects of differing gel volumes on pharmacokinetics (PK). IQB4012, a gel containing the non-nucleoside reverse transcriptase inhibitor IQP-0528 and tenofovir (TFV), was applied to the pigtailed macaque vagina and rectum. Vaginal gel volumes (1% loading of both drugs) were 0.5 or 1.5 ml; following...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0538-0
更新日期：2018-10-01 00:00:00
abstract：:Lipid-based liquid crystalline (LC) systems have the potential to sustain the oral absorption of poorly water-soluble drugs in vivo, facilitating slow drug release from their complex internal structure. To further evaluate the dynamic relationship between gastric retention and sustained drug absorption for these syste...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-015-0253-z
更新日期：2015-12-01 00:00:00
abstract：:The present research work summarises the development of an in situ gelling ophthalmic nanoemulsion of brinzolamide providing sustained release and prolonged therapeutic effect for the treatment of glaucoma. Nanoemulsions were prepared using castor oil, polyoxyl 35 castor oil and polysorbate 80 and with gellan gum as t...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-019-00697-0
更新日期：2020-04-01 00:00:00
abstract：:This review focuses on clinical application of intravaginal formulations containing nitric oxide (NO). Poly(D,L-lactic acid-co-glycolic acid)-based microparticles or nanoparticles encapsulated with nitric oxide prodrugs, such as diethylenetriamine diazeniumdiolate and S-nitrosoglutathione, have been developed for the ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-011-0026-2
更新日期：2011-06-01 00:00:00
abstract：:Nanoparticulate systems have emerged as prevalent drug delivery systems over the past few decades. These delivery systems (such as liposomes, emulsions, nanocrystals, and polymeric nanocarriers) have been extensively used to improve bioavailability, prolong pharmacological effects, achieve targeted drug delivery, as w...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-013-0129-z
更新日期：2013-10-01 00:00:00
abstract：:Gemcitabine is used as a first-line drug for treating many solid tumours. However, it suffers from a major drawback of strong side effects and short plasma half-life because of degradation by enzyme when administered intravenously. Polyesters and copolyesters are the most widely used and preferred class of biodegradab...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0372-9
更新日期：2017-06-01 00:00:00
abstract：:The tissue distribution and percutaneous drug absorption of indomethacin (IND) patches were studied using commercial IND as a comparison. The concentration of IND in skin, plasma, and muscle in mice was measured by LC-MS/MS, and the IND concentration in the dermis of rats was also monitored by microdialysis. After per...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0392-5
更新日期：2017-10-01 00:00:00
abstract：:The objective of the present work was to develop polymeric nanoparticles of uricase and aceclofenac (NSAID) and to incorporate them into gel, for delivering drugs to synovial joints, for effective treatment of Gout. Nanoparticles containing uricase and aceclofenac were prepared by double emulsion solvent evaporation m...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-015-0219-1
更新日期：2015-06-01 00:00:00
abstract：:Nanotechnology is expected to revolutionize existing drug delivery. Many nanostructured systems have been employed for drug delivery and yielded some promising results. Solid lipid nanoparticles (SLN) have been looked at as a potential drug carrier system since last two decades. SLN do not show biotoxicity as they are...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-012-0088-9
更新日期：2012-08-01 00:00:00
abstract：:In vivo toxicity and absorption studies of topical ocular drugs are problematic, because these studies involve invasive tissue sampling and toxic effects in animal models. Therefore, different human corneal models ranging from simple monolayer cultures to three-dimensional models have been developed for toxicological ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-016-0330-y
更新日期：2016-12-01 00:00:00
abstract：:Wound healing is a physiological event that generates reconstitution and restoration of granulation tissue that ends with scar formation. As omega fatty acids are part of membrane phospholipids and participate in the inflammatory response, we investigated the effects of omega-3, omega-6, and omega-9 fatty acids in the...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0522-8
更新日期：2019-04-01 00:00:00
abstract：:Curcumin, resveratrol, and thymoquinone are the potential natural bio-actives reported with good anti-psoriatic activity. However, poor aqueous solubility and limited skin permeation of these natural bio-actives hinder their effective delivery and potential therapeutic outcome. In this regard, current research work fo...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00852-y
更新日期：2020-09-23 00:00:00
abstract：:Chemical injury by alkali burn is a major cause of corneal blindness in the clinical setting. Current management advocates multiple therapies aimed to prevent inflammation, initiate quick re-epithelialization, arrest the fibrosis, and avoid dry eye and pain by using bandage contact lenses. We hypothesized sustained de...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0541-5
更新日期：2018-10-01 00:00:00
abstract：:Simvastatin (SIM) is a commonly used cholesterol-lowering drug that can reduce the risk of major cardiovascular events. However, due to its poor intrinsic water solubility, the drug is poorly absorbed from the gastrointestinal tract and exhibits a low oral bioavailability of approximately 5%. The aim of this study was...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00853-x
更新日期：2020-09-11 00:00:00
abstract：:The promise of RNA interference (RNAi) technology in cancer therapeutics aims to deliver small interfering RNA (siRNA) for silencing of gene expression in cell type-specific pathway. However, the challenge for the delivery of stable siRNA is hindered by an immune-hostile tumor microenvironment and physiological barrie...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-016-0352-5
更新日期：2017-04-01 00:00:00
abstract：:The purpose of this study was to explore poly(vinylpyrrolidone-co-vinyl acetate) (PVP VA64) as a novel release-modifier to tailor the drug release from ethylcellulose (EC)-based mini-matrices prepared via hot melt extrusion (HME). Quetiapine fumarate (QF) was selected as model drug. QF/EC/PVP VA64 mini-matrices were e...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0437-9
更新日期：2018-12-01 00:00:00
abstract：:We previously showed that the combination of the non-nucleoside reverse transcriptase inhibitor (NNRTI) MIV-150 with zinc acetate (ZA) formulated in a carrageenan (CG; MZC) gel provided macaques significant protection against vaginal simian-human immunodeficiency virus-RT (SHIV-RT) challenge, better than either MIV-15...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0421-4
更新日期：2017-12-01 00:00:00
abstract：:Intranasal administration of mucus-penetrating nanoparticles is an emerging trend to increase drug delivery to the brain. In order to overcome rapid nasal mucociliary clearance, low epithelial permeation, and local enzymatic degradation, we investigated the influence of PEGylation on nose-to-brain delivery of polycapr...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00816-2
更新日期：2020-12-01 00:00:00
abstract：:The protective effects of synthetic lung surfactant Exosurf® (containing cetyl alcohol) against endotoxin-induced inflammation have been demonstrated in the literature. Thus, it is envisioned that nanoparticles loaded with quercetin (Q-NPs) prepared with binary mixtures of cetyl alcohol (CA) and Gelucire 44/14® (geluc...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-013-0130-6
更新日期：2013-08-01 00:00:00
