Abstract：
:How prevalent are peptide therapeutic products? How innovative are the formulations used to deliver peptides? This review provides a critical analysis of therapeutic peptide products and the formulations approved by the United States Food and Drug administration (FDA), the European Medicines Agency (EMA), and the Japanese Pharmaceuticals and Medical Devices Agency (PMDA). This review also provides an in-depth analysis of dosage forms and administration routes for delivering peptide therapeutics, including injectables, oral dosage forms, and other routes of administration. We discuss the function of excipients in parenteral formulations in detail, since most peptide therapeutics are parenterally administered. We provide case studies of alternate delivery routes and dosage forms. Based on our analysis, therapeutic peptides administered as injectables remain the most commonly used dosage forms, particularly in the form of subcutaneous, intravenous, or intramuscular injections. In addition, therapeutic peptides are formulated to achieve prolonged release, often through the use of polymer carriers. The limited number of oral therapeutic peptide products and their poor absorption and subsequent low bioavailability indicate a need for new technologies to broaden the formulation design space. Therapeutic peptide products may also be delivered through other administration routes, including intranasal, implant, and sublingual routes. Therefore, an in-depth understanding of how therapeutic peptides are now formulated and administered is essential to improve peptide delivery, improve patient compliance, and reduce the healthcare burden for these crucial therapeutic agents.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Zhang Y,Zhang H,Ghosh D,Williams RO 3rddoi
10.1016/j.ijpharm.2020.119491subject
Has Abstractpub_date
2020-09-25 00:00:00pages
119491eissn
0378-5173issn
1873-3476pii
S0378-5173(20)30475-0journal_volume
587pub_type
杂志文章,评审abstract：:There is a growing interest in drug-phospholipid complexes and similar formulations that are mostly solid dispersions with high drug load. This study aims to explore the feasibility of such phospholipid-based solid dispersions as well as to characterize them. A particular aim was to compare monoacyl phosphatidylcholin...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.06.039
更新日期：2015-08-01 00:00:00
abstract：:Three novel amino acid based anionic amphiphilic copolymers poly(sodium N-acryloyl-l-valinate-co-alkylacrylamide) (where, alkyl=octyl and dodecyl) with either 9 or 16 mol% hydrophobic substitution were synthesized. These hydrophobically modified polyelectrolytes (HMPs), above a critical concentration, self-assemble in...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.01.041
更新日期：2011-04-04 00:00:00
abstract：:The transmucosal routes such as pulmonary, nasal and oral routes are most important and common routes for drug delivering to the body. However, peptide and protein drugs are degraded before they reach the blood stream and cannot cross the mucosal barriers. The mucoadhesive polymer-coated nanoparticles colloidal carrie...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.02.031
更新日期：2006-06-19 00:00:00
abstract：:Chitosan/biomimetic apatite thin films were grown in mild conditions of temperature and pressure by Combinatorial Matrix-Assisted Pulsed Laser Evaporation on Ti, Si or glass substrates. Compositional gradients were obtained by simultaneous laser vaporization of the two distinct material targets. A KrF* excimer (λ=248n...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.07.015
更新日期：2016-09-10 00:00:00
abstract：:This opinion piece gives reasons for high dose DPI applications, points out challenges and shows opportunities and possible solutions for high dose DPI. This piece of work shall set the stage for more in-depth reviews of state of the art and research papers addressing the challenges of high dose DPI which shall be inc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.06.038
更新日期：2018-09-05 00:00:00
abstract：:Superdisintegrants are a key excipient used in immediate release formulations to promote fast tablet disintegration, therefore understanding the impact of superdisintegrant variability on product performance is important. The current study examined the impact of superdisintegrant critical material attributes (viscosit...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119080
更新日期：2020-03-15 00:00:00
abstract：:The aim of the present study was to develop a semi-empirical mathematical model, which is able to predict the release profiles of solid lipid extrudates of different dimensions. The development of the model was based on the application of ANNs and GP. ANNs' abilities to deal with multidimensional data were exploited. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.05.021
更新日期：2012-10-15 00:00:00
abstract：:The aim of the present work was to find a suitable method for the introduction of thiol functions on the surface of poly(DL-lactic acid) (PLA) nanoparticles. Three different approaches were investigated. The modification of the surface involves the activation of PLA carboxylic acid groups followed by the attack of a n...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00542-2
更新日期：2003-01-16 00:00:00
abstract：:Three-dimensional printing (3DP) is a highly disruptive technology with the potential to change the way pharmaceuticals are designed, prescribed and produced. Owing to its low cost, diversity, portability and simplicity, fused deposition modeling (FDM) is well suited to a multitude of pharmaceutical applications in di...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.07.024
更新日期：2018-09-05 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：:Oridonin (ORI), a diterpenoid compound with promising antitumor activity, was proved to possess potent antileukemia efficacies in vitro and in vivo recently. However, the development and application of ORI was limited by its poor solubility and rapid plasma clearance. The purpose of this study was to solve these probl...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.08.014
更新日期：2013-11-01 00:00:00
abstract：:The effects of addition of divalent cations and phosphate buffer on the degree of beta-carotene encapsulation in a mannitol matrix during freeze-drying were analyzed. The degradation rate of encapsulated beta-carotene as a function of % RH and its relationship with the physical state of the matrix during storage at 25...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.023
更新日期：2007-03-06 00:00:00
abstract：:Regional drug delivery via dry powder inhalers offers many advantages in the management of pharmaceutical compounds for the prevention and treatment of respiratory diseases. In the present study, doxorubicin (DOX)-loaded nanoparticles were incorporated as colloidal drug delivery system into inhalable carrier particles...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.03.052
更新日期：2006-08-17 00:00:00
abstract：:Integrin alpha(5)beta(1) is expressed on several types of cancer cells, including colon cancer, and plays an important role in tumor growth and metastasis. The ability to target the integrin alpha(5)beta(1) using an appropriate drug delivery nano-vector can significantly help in inhibiting tumor growth, reducing tumor...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.09.016
更新日期：2009-01-21 00:00:00
abstract：:The apparent diffusion coefficients, Dapp, and the release mechanisms of salicylic acid from salicylic acid-loaded polyacrylamide hydrogels, SA-loaded PAAM, and salicylic acid-doped poly(phenylene vinylene)/polyacrylamide hydrogels, SA-doped PPV/PAAM, were investigated. In the absence of an electric field, the diffusi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.12.032
更新日期：2009-04-17 00:00:00
abstract：:Drug interactions with diosmectite, a gastric-protective drug, were studied in vitro using an artificial stomach-duodenum model. The behavior of neutral and ionisable drugs with pKa values ranging between 2 and 8 was monitored to determine the physicochemical characteristics of the interactions. The main neutral (digo...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00073-3
更新日期：1999-05-10 00:00:00
abstract：:Matrix metalloproteinases (MMPs) overexpression plays a critical role in cancer invasion and metastasis. We utilized this key feature of tumor microenvironment to develop a disease-stimuli triggered drug delivery system. Poly(acrylic acid) hydrogels were synthesized by UV polymerization and pendant MMP-2 sensitive pep...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.03.012
更新日期：2012-06-15 00:00:00
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 rea...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2016.05.065
更新日期：2016-11-30 00:00:00
abstract：:This work examines the influence of essential oil composition on emulsification with rhamnolipids and their use as therapeutic antimicrobial agents against two opportunistic pathogens, methicillin-resistant Staphylococcus aureus (MRSA) and Candida albicans. Rhamnolipids, produced by Pseudomonas aeruginosa, with waste ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.09.039
更新日期：2014-12-10 00:00:00
abstract：:Raman spectroscopy may be implemented through a microscope to provide fine scale axial and lateral chemical maps. The molecular structure of many drugs makes Raman spectroscopy particularly well suited to the investigation of pharmaceutical systems. Chemometric methods currently used to assess bulk Raman spectroscopic...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2010.12.030
更新日期：2011-09-30 00:00:00
abstract：:Heart failure still represents the leading cause of death worldwide. Novel strategies using stem cells and growth factors have been investigated for effective cardiac tissue regeneration and heart function recovery. However, some major challenges limit their translation to the clinic. Recently, biomaterials have emerg...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2016.10.061
更新日期：2017-05-25 00:00:00
abstract：:An increasing elderly population is leading to a change in the global demographics. This presents a new challenge to society and the pharmaceutical industry. This demographic shift is providing an opportunity for the pharmaceutical industry to meet the specific needs of the changing patient population. One issue that ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2016.03.008
更新日期：2016-10-30 00:00:00
abstract：:Thermoreversible nasal gels of Vitamin B(12) using pluronic PF 127 were aimed to improve absorption and patient compliance. In the present research work, effects of Vitamin B(12) and gel additives, viz. PF concentration, osmolarity, polyethylene glycol (PEG 15000) on thermodynamic properties of phase transitions at ge...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2003.10.005
更新日期：2004-02-11 00:00:00
abstract：:The absorption mechanism of several penicillins was characterized using in situ single-pass intestinal perfusion in the rat. The intrinsic membrane parameters were determined using a modified boundary layer model (fitted value +/- S.E.): Jmax* = 11.78 +/- 1.88 mM, Km = 15.80 +/- 2.92 mM, Pm* = 0, Pc* = 0.75 +/- 0.04...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/0378-5173(92)90147-t
更新日期：1992-09-20 00:00:00
abstract：:The chemical potentials of drug-polymer electrostatic interaction have been utilized to develop a novel ternary chitosan-ibuprofen-gellan nanogel as controlled transdermal delivery tool for ibuprofen. The ternary nanogels were prepared by a combination of electrostatic nanoassembly and ionic gelation techniques. The e...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.05.030
更新日期：2015-07-25 00:00:00
abstract：:A series of labdans and their derivatives have been identified as novel potential antileishmanial drugs using an in vitro test system against extracellular promastigotes and intracellular amastigotes of Leishmania donovani in murine macrophages (Kayser, O., Kiderlen, A.F., 1998. In vitro activity of leishmanicidal lab...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00434-2
更新日期：2000-03-10 00:00:00
abstract：:Currently, the compressed tablet and its oral administration is the most popular drug delivery modality in medicine. The accurate porosity and tensile strength characterization of a tablet design is vital for predicting its performance such as disintegration, dissolution, and drug-release efficiency upon administratio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.03.018
更新日期：2018-05-05 00:00:00
abstract：:Squamous cell carcinoma treatment has limited therapeutic options and the incidence rate is increasing recently. In the present investigation, we developed poly(lactic-co-glycolic acid) (PLGA) nanopatterned films (NPFs) through poly dimethyl siloxane (PDMS) cast molding technique and explored its therapeutic efficacy ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119100
更新日期：2020-03-30 00:00:00
abstract：:Microneedle systems have gained attention as having many advantages over transdermal patches and hypodermic needles. The procedure provides adequate skin permeation rates without pain or severe infection. To obtain information for designing a microneedle system, macroneedles were used instead of microneedles to invest...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.02.046
更新日期：2006-06-19 00:00:00
abstract：:A series of mesocellular foams (MCFs)-based mesoporous silica nanospheres (DH-MCF-P123-n, (n=12, 2, 0.5)) were synthesized as controlled-release deliveries for a typical antidepressant drug, venlafaxine. The foams were 3-(2,3-dihydroxypropoxyl)propyl-grafted and the P123 template partially preserved. We studied the re...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.12.048
更新日期：2012-03-15 00:00:00
