Abstract：
:Topical formulations aim to target the skin for a variety of cosmetic, protective or therapeutic needs. Despite the use of creams and ointments over the millennia, the bioavailability of actives from topical preparations remains quite low, often not exceeding 1-2% of the applied dose. In this review we examine the reasons underlying the poor performance of topical preparations. We also outline a rational approach, based on Fick's laws of diffusion, to develop advanced topical formulations. Methodologies which are currently used in research and development are critically examined and the importance of understanding the fate of the vehicle as well as the active is emphasised. Advanced topical formulation development will also be facilitated by emerging and sophisticated analytical techniques that are able to probe real time delivery of actives to the skin. A good understanding of the underlying physical chemistry of both the formulation and the skin is crucial in the development of optimised topical products.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Hadgraft J,Lane MEdoi
10.1016/j.ijpharm.2016.05.065subject
Has Abstractpub_date
2016-11-30 00:00:00pages
52-57issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(16)30455-0journal_volume
514pub_type
杂志文章,评审abstract：:Subcutaneous vaccination of C57bl/6 mice with irradiated B16 melanoma cells supplemented with liposomal interleukin-2 (IL2) or murine interferon-gamma (mIFNgamma), resulted in systemic protection in 50% of the animals, against a subsequent tumor cell challenge in a dose dependent manner. The protective efficacy was co...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00039-3
更新日期：1999-06-10 00:00:00
abstract：:PLGA microspheres undergo physical ageing but their ageing kinetics have not been reported, nor the effect of encapsulated protein or plasmid DNA on any associated changes to the glass transition. Differential scanning calorimetry (DSC) was used to measure the rate of ageing of various PLGA microsphere formulations, w...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.02.026
更新日期：2007-07-18 00:00:00
abstract：:A new set of 142 experimentally determined complexation constants between sulfobutylether-β-cyclodextrin and diverse organic guest molecules, and 78 observations reported in literature, were used for the development of the QSPR models by the two machine learning regression methods - Cubist and Random Forest. Similar m...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.03.065
更新日期：2011-10-14 00:00:00
abstract：:The development of vaccine delivery systems that will remove or reduce the need for repeated dosing has led to the investigation of sustained release systems. In this context, the duration of antigen release is of great importance as is the requirement for concomitant adjuvant release. In this work, lipid implants con...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.06.052
更新日期：2015-09-30 00:00:00
abstract：:Virus-like particles (VLPs) have been exploited for various biomedical applications, such as the monitoring, prevention, diagnosis and therapy of disease. In this study, a novel multifunctional VLPs nanocarrier (TK-VLPs) was prepared and used for tumor-targeted delivery. The SPR and cell uptake results indicated that ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.02.037
更新日期：2016-04-11 00:00:00
abstract：BACKGROUND:Pulmonary administration of the antimicrobial drugs colistin sulphomethate and tobramycin has been shown to be effective in slowing down pulmonary deterioration in cystic fibrosis (CF) patients. Both drugs are administered by liquid nebulisation, a technique known to have disadvantages. Dry powder inhalation...
journal_title：International journal of pharmaceutics
pub_type： 临床试验,杂志文章
doi：10.1016/j.ijpharm.2006.11.021
更新日期：2007-04-20 00:00:00
abstract：:Many medicines prescribed for children are unlicensed. Solid dosage forms present problems as children have difficulty swallowing whole tablets or capsules. When medicines are not licensed for children, it is unlikely that there will be a suitable, licensed liquid formulation and so extemporaneous liquid preparations ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.05.006
更新日期：2005-08-26 00:00:00
abstract：:In the 1990s chitosan turned out to be a useful excipient in various pharmaceutical formulations. By modifications of the primary amino group at the 2-position of this poly(beta1-->4 D-glucosamine), the features of chitosan can even be optimised according to a given task in drug delivery systems. For peroral peptide d...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/s0378-5173(99)00365-8
更新日期：2000-01-20 00:00:00
abstract：:Extrusion-spheronisation was used to generate smooth, highly spherical granules of a microcrystalline cellulose/propyl gallate/water paste. Freeze-drying retained the shape and size of the granules, whereas oven-drying produced roughened granules due to the uneven shrinkage of the wet powders. Compaction of one size f...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.050
更新日期：2007-03-06 00:00:00
abstract：:A comprehensive model is proposed to accurately describe drug release kinetics from a coated plane sheet when drug loading in the core is above its saturation level. The general solutions are acquired in a dimensionless form by the Laplace transform and the solution for the special case-a perfect sink condition, is de...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00373-7
更新日期：2000-03-20 00:00:00
abstract：:Developments in the field of molecular oncology have revealed that resistance to chemotherapeutics is acqured through several mechanisms including overexpression of common oncogenic proteins. Signal Transducer and Activator of Transcription 3 (STAT3) is one of these oncogenes that is overexpressed in many cancer types...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.04.034
更新日期：2017-06-15 00:00:00
abstract：:Formulation of poorly water-soluble drugs in the most stable dosage form for oral delivery perhaps presents the greatest challenge to pharmaceutical industry. Physical transformation of drug substance into its more soluble but metastable amorphous form is one of the approaches for improving dissolution rate of such dr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.06.009
更新日期：2004-09-10 00:00:00
abstract：:Insulin (INS) was incorporated into complexes with the block polyelectrolyte quaternized poly[3,5-bis(dimethylaminomethylene)hydroxystyrene]-b-poly(ethylene oxide) (QNPHOSEO), which is a cationic-neutral block polyelectrolyte. Light scattering techniques are used in order to examine the size, the size distribution and...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.06.013
更新日期：2015-08-01 00:00:00
abstract：:Cell replacement therapy is a widely discussed novel concept of medical treatment. The increased knowledge in the stem cell field, particularly pluripotent stem cells, potentially provides powerful tools for this therapeutic concept. A large number of disease characterized by the loss of functional cells are potential...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2009.03.003
更新日期：2009-11-03 00:00:00
abstract：:The aim of this study was to evaluate the transdermal permeation enhancement of N-trimethyl chitosan (TMC) with different degrees of quaternization (DQ). TMCs with DQ of 40 and 60% (TMC40 and TMC60) were synthesized and characterized by (1)H NMR. Testosterone (TS) used as an effective drug, four different gels were pr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.12.050
更新日期：2008-05-22 00:00:00
abstract：:This study systematically demonstrated the antigenicity kinetics of HBV vaccine microneedles (MNs) during the fabrication, application and storage. To improve the stability of HBsAg in a microneedle patch, several selected saccharides were added to the MN formulations as stabilizers. According to the experimental data...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118489
更新日期：2019-08-15 00:00:00
abstract：:Changes in the rheological properties of four o/w cream formulations differing in the combination of surfactants were studied. The non-ionic surfactants used were soybean derivatives, polyethylene glycol 10 and 25 soya sterol, and sorbitol derivatives, sorbitan monooleate and trioleate. Combinations of the soybean and...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00675-5
更新日期：2001-06-19 00:00:00
abstract：:Polyamidoamine-polylysine graft copolymers (PAMAM-g-PLL) were prepared by ring-opening polymerization of benzyloxycarbonyl lysine N-carboxyanhydride (Lys(Z)-NCA) initiated with primary amine of generation 4 polyamidoamine (PAMAM G4) and subsequent deprotection of polyamidoamine-poly-(benzyloxycarbonyl lysine) copolyme...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.08.036
更新日期：2011-11-28 00:00:00
abstract：:Amphotericin B (AmB) has a broad antifungal and leishmanicidal activity with low incidence of clinical resistance. Its parenteral administration has high risk of nephrotoxicity that limits its use. In order to treat cutaneous infections, AmB topical administration is a safer therapy because of the low systemic absorpt...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.07.004
更新日期：2014-10-01 00:00:00
abstract：:A novel, efficient delivery system for iron (Fe2+) was developed using the alginate biopolymer. Iron loaded alginate nanoparticles were synthesized by a controlled ionic gelation method and was characterized with respect to particle size, zeta potential, morphology and encapsulation efficiency. Successful loading was ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.09.053
更新日期：2016-11-20 00:00:00
abstract：:To examine the relative contributions of molecular mobility and thermodynamic factor, the relationship between glass transition temperature (T(g)) and the crystallization rate was examined using amorphous dihydropyridines (nifedipine (NFD), m-nifedipine (m-NFD), nitrendipine (NTR) and nilvadipine (NLV)) with differing...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.11.052
更新日期：2007-05-04 00:00:00
abstract：:Tumor growth and metastasis are multistep processes regulated by multiple signaling pathways. The successful treatment of cancer largely depends on the ability to inhibit metastatic process. Multiphase inhibition of metastasis is a promising approach. Here, we described a targeting delivery system which was constructe...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119085
更新日期：2020-03-15 00:00:00
abstract：:Marinosomes are liposomes based on a natural marine lipid extract containing a high polyunsaturated fatty acid (PUFA) ratio. They were prepared and characterized in conditions that mimic that of topical application in terms of pH, temperature and calcium. Marinosomes were stable in storage conditions for 1 month. At l...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00217-x
更新日期：2002-08-21 00:00:00
abstract：:Aerosolization behavior of carrier-free l-leucine coated salbutamol sulphate inhalable powders has been studied. L-Leucine coatings were formed by physical vapour deposition (PVD) on the surface of the spherical particles in the gas phase. While depositing L-leucine formed pointy crystalline asperities whose size and ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.08.017
更新日期：2009-01-05 00:00:00
abstract：:In this study, we evaluated the palatability of orally disintegrating tablets (ODTs) containing core granules with different particle sizes, coating, and types of materials using visual analog scales (VAS). Tableting the core granules into ODTs reduced rough mouth feel and improved overall palatability compared to the...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ijpharm.2015.02.023
更新日期：2015-04-30 00:00:00
abstract：:The enhancing effects of non-ionic surfactants on the permeation of piroxicam from the poloxamer gels were evaluated using Franz diffusion cells fitted with excised rat skins. The effectiveness of penetration enhancers, the ratio of piroxicam flux in the presence or absence of enhancers, was defined as the enhancement...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00699-8
更新日期：2001-07-17 00:00:00
abstract：:The aim of this study was to elucidate the importance of potential limited solubility effects for the control of drug release from hydrophilic matrix tablets loaded with a freely water-soluble drug. It is often assumed that the considerable amounts of water penetrating into this type of advanced drug delivery systems ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.05.001
更新日期：2017-06-30 00:00:00
abstract：:In the present study, two indices of acute intestinal permeability changes were investigated as measurements of drug induced intestinal damage. The first method was based on 14C-polyethylene glycol (PEG) 4000 permeability assessment and the second was based on histological evaluation of the intestine. The test compoun...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.01.009
更新日期：2006-04-07 00:00:00
abstract：:In this study, the roll compaction of an intermediate drug load formulation was performed using horizontally and vertically force fed roll compactors. The horizontally fed roll compactor was equipped with an instrumented roll technology allowing the direct measurement of normal stress at the roll surface, while the ve...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.02.042
更新日期：2015-04-30 00:00:00
abstract：:The cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE2) pathway plays an important role in tumor development and formation of metastases. It was earlier reported that cyclodextrin derivatives have a high affinity to form complexes with PGE2. Based on these results radiolabeled cyclodextrins - as new radiopharmaceuticals ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118954
更新日期：2020-02-25 00:00:00
