Did you know ? If you order before Friday 14h we deliver 90PCT of the the time next Tuesday, GENTAUR another in time delivery

Pubmed ID :28286315
Publication Date : //

Formulation of hydrophobic peptides for skin delivery via coated microneedles.


Microneedles (MNs) have been investigated as a minimally-invasive delivery technology for a range of active pharmaceutical ingredients (APIs). Various formulations and methods for coating the surface of MNs with therapeutics have been proposed and exemplified, predominantly for hydrophilic drugs and particulates. The development of effective MN delivery formulations for hydrophobic drugs is more challenging with dosing restrictions and the use of organic solvents impacting on both the bioactivity and the kinetics of drug release. In this study we propose a novel formulation that is suitable for MN coating of hydrophobic auto-antigen peptides currently being investigated for antigen specific immunotherapy (ASI) of type 1 diabetes. The formulation, comprising three co-solvents (water, 2-methyl-2-butanol and acetic acid) and polyvinylalcohol 2000 (PVA2000) can dissolve both hydrophilic and hydrophobic peptide auto-antigens at relatively high, and clinically relevant, concentrations (25mg/ml or 12.5mg/ml). The drug:excipient ratio is restricted to 10:1 w/w to maximise dose whilst ensuring that the dry-coated payload does not significantly impact on MN skin penetration performance. The coating formulation and process does not adversely affect the biological activity of the peptide. The delivery efficiency of the coated peptide into skin is influenced by a number of parameters. Electropolishing the metal MN surface increases delivery efficiency from 2.0±1.0% to 59.9±6.7%. An increased mass of peptide formulation per needle, from 0.37μg to 2μg peptide dose, resulted in a thicker coating and a 20% reduction in the efficiency of skin delivery. Other important performance parameters for coated MNs include the role of excipients in assisting dissolution from the MNs, the intrinsic hydrophobicity of the peptide and the species of skin model used in laboratory studies. This study therefore both exemplifies the potential of a novel formulation for coating hydrophobic and hydrophilic peptides onto MN devices and provides new insight into the factors that influence delivery efficiency from coated MNs. Importantly, the results provide guidance for identifying critical attributes of the formulation, coating process and delivery device, that confer reproducible and effective delivery from coated MNs, and thus contribute to the requirements of the regulators appraising these devices.

Authors : Zhao Xin , Coulman Sion A , Hanna Stephanie J , Wong F Susan , Dayan Colin M , Birchall James C ,

Related products :

Catalog number Product name Quantity
506-25 NuGel™ P-Phenyl, Polymer Coated Hydrophobic Support 25 Grams
502-100 NuGel™ P-Octyl, Polymer Coated Hydrophobic Support 100 Grams
506-100 NuGel™ P-Phenyl, Polymer Coated Hydrophobic Support 100 Grams
502-25 NuGel™ P-Butyl, Polymer Coated Hydrophobic Support 25 Grams
502-100 NuGel™ P-Butyl, Polymer Coated Hydrophobic Support 100 Grams
502-25 NuGel™ P-Octyl, Polymer Coated Hydrophobic Support 25 Grams
Skin - SKT961 Skin tumor tissue array consists of 36 duplicated cases of skin tumors and 12 cases of normal and other non_malignant skin tissues. 1.5mm
Skin - SKD241 Skin disease tissue array, 24 cases of normal, reactive and tumor tissues of the skin 2.5mm
Z7020093 Skin Tumor Tissue Array - 36 duplicated cases of skin tumors and 12 cases of normal and other non-malignant skin tissues
Z7020093 Skin Tumor Tissue Array _ 36 duplicated cases of skin tumors and 12 cases of normal and other non_malignant skin tissues 5 slides
Z7020093 Skin Tumor Tissue Array - 36 duplicated cases of skin tumors and 12 cases of normal and other non-malignant skin tissues 5 slides
Z7020093 Skin Tumor Tissue Array _ 36 duplicated cases of skin tumors and 12 cases of normal and other non_malignant skin tissues 5 slides
KP1342 Pep - 1: Chariot (Non - Covalent Delivery of Peptides and Proteins) 1 mg
ACT-IPST10 BluPower™ Coomassie Stain, properiatary formulation 10x 250ml for 40-60 gels
ACT-ID1591 QuickRun™ Fast electrophoresis buffer 10X, proprietary formulation, 1L of 10x Conc. 10 units
AG066-1D DryCoat Assay Stabilizer _ Dry Formulation _ No added protein..Reconstitute w_ 1 L DI water
80061 ELISA Plate Blocking Buffer concentrate (10X) Gelatin-based (translucent formulation) 100 ml
80063 ELISA Plate Blocking Buffer concentrate (10X) milk-based (translucent formulation) 100 ml
80061 ELISA Plate Blocking Buffer concentrate (10X) Gelatin-based (translucent formulation) Species Reactivity: 100 ml Product tipe: Buffer
80063 ELISA Plate Blocking Buffer concentrate (10X) milk-based (translucent formulation) Species Reactivity: 100 ml Product tipe: Buffer
Z5070008 [DISCONTINUED] Skin Tumor Tissue Array _ Skin Malignant melanoma 5 slides
PEA081 FRESH SKIN (minimum order: 25cm2) Cynomolgus Monkey skin 1 cm2
Z5070008 [DISCONTINUED] Skin Tumor Tissue Array _ Skin Malignant melanoma 5 slides
PEA079 FRESH SKIN (minimum order: 25cm2) Beagle dog skin 1 cm2
PEA030 FRESH SKIN (minimum order: 25cm2) xx minipig skin 1 cm2


 

GENTAUR Belgium BVBA BE0473327336
Voortstraat 49, 1910 Kampenhout BELGIUM
Tel 0032 16 58 90 45

Fax 0032 16 50 90 45
info@gentaur.com | Gentaur





GENTAUR Ltd.
Howard Frank Turnberry House
1404-1410 High Road
Whetstone London N20 9BH
Tel 020 3393 8531 Fax 020 8445 9411
uk@gentaur.com | Gentaur

 

 




GENTAUR France SARL
9, rue Lagrange, 75005 Paris
Tel 01 43 25 01 50

Fax 01 43 25 01 60
RCS Paris B 484 237 888

SIRET 48423788800017

BNP PARIBAS PARIS PL MAUBERT BIC BNPAFRPPPRG

france@gentaur.com | Gentaur

GENTAUR GmbH
Marienbongard 20
52062 Aachen Deutschland
Support Karolina Elandt
Tel: 0035929830070
Fax: (+49) 241 56 00 47 88

Logistic :0241 40 08 90 86
Bankleitzahl 39050000
IBAN lautet DE8839050000107569353
Handelsregister Aachen HR B 16058
Umsatzsteuer-Identifikationsnummer *** DE 815175831
Steuernummer 201/5961/3925
de@gentaur.com | Gentaur

GENTAUR U.S.A
Genprice Inc, Logistics
547, Yurok Circle
San Jose, CA 95123
CA 95123
Tel (408) 780-0908,
Fax (408) 780-0908,
sales@genprice.com

Genprice Inc, Invoices and accounting
6017 Snell Ave, Ste 357
San Jose, CA 95123




GENTAUR Nederland BV
NL850396268B01 KVK nummer 52327027
Kuiper 1
5521 DG Eersel Nederland
Tel:  0208-080893  Fax: 0497-517897
nl@gentaur.com | Gentaur
IBAN: NL04 RABO 0156 9854 62   SWIFT RABONL2U






GENTAUR Spain
tel:0911876558
spain@gentaur.com | Gentaur






ГЕНТАУЪР БЪЛГАРИЯ
ID # 201 358 931 /BULSTAT
София 1000, ул. "Граф Игнатиев" 53 вх. В, ет. 2
Tel 0035924682280 Fax 0035924808322
e-mail: Sofia@gentaur.com | Gentaur
IBAN: BG11FINV91501014771636
BIC: FINVBGSF

GENTAUR Poland Sp. z o.o.


ul. Grunwaldzka 88/A m.2
81-771 Sopot, Poland
TEL Gdansk 058 710 33 44 FAX  058 710 33 48              

poland@gentaur.com | Gentaur

Other countries

Österreich +43720880899

Canada Montreal +15149077481

Ceská republika Praha +420246019719

Danmark +4569918806

Finland Helsset +358942419041

Magyarország Budapest +3619980547

Ireland Dublin+35316526556

Luxembourg+35220880274

Norge Oslo+4721031366

Sverige Stockholm+46852503438

Schweiz Züri+41435006251

US New York+17185132983

GENTAUR Italy
SRL IVA IT03841300167
Piazza Giacomo Matteotti, 6
24122 Bergamo Tel 02 36 00 65 93
Fax 02 36 00 65 94
italia@gentaur.com | Gentaur