Transdermal nortriptyline hydrocloride patch formulated within a chitosan matrix intended to be used for smoking cessation.
OBJECTIVE
The aim of this study was to prepare and characterize both physically and biopharmaceutically, a nortriptyline hydrochloride (NTP-HCl) patch formulated in chitosan.


METHODS
16 g of each chitosan patch formulation (I, II and III, see Table 1 ) was poured onto rectangular glass plates (64 cm²) at a height of 1 mm and dried for 24 h at room temperature. In order to characterize the chitosan patches, polarized microscopy, in vitro skin permeation studies by passive diffusion and iontophoresis and rheological and bioadhesion studies were performed.


RESULTS
Polarized microscopy revealed the absence of aggregates and crystal forms of NTP-HCl in all transdermal patches after 30 days of storage. The rheological behavior of Patches I, II and III was predominantly elastic. The low level of adhesion of Patch III (containing PF-127 + 1-dodecanol) could be a result of the interactions between chitosan and PF-127 in the presence of 1-dodecanol. Patches I and II had approximately the same value of adhesion (≈ 60 mN.mm). The transdermal patch with chitosan, PF-127 and 1-dodecanol (Patch III) provided a reasonable flux of NTP-HCl across the skin compared with Patches I and II. Iontophoresis applied to the patches did not increase the penetration of NTP-HCl across the skin.


CONCLUSIONS
The data suggest that Patch III is suitable for use in clinical practice pending further studies.
Departamento de Farmacia y Tecnología Farmacéutica, Universidad de Valencia, Av. Vicente Andrés Estellés s/n, Burjassot, Valencia, Spain. josejuanescobarchavez@gmail.com
José Juan
JJ
Escobar-Chávez
Virginia
V
Merino
Octavio
O
Díez-Sales
Amparo
A
Nácher-Alonso
Adriana
A
Ganem-Quintanar
Marina
M
Herráez
Matilde
M
Merino-Sanjuán
D018759:Adrenergic Uptake Inhibitors / Q000008:administration & dosage*; D000328:Adult; D000929:Antidepressive Agents, Tricyclic / Q000008:administration & dosage*; D048271:Chitosan / Q000737:chemistry*; D005260:Female; D006801:Humans; D007478:Iontophoresis; D008875:Middle Aged; D009661:Nortriptyline / Q000008:administration & dosage*; D012867:Skin / Q000378:metabolism; D016540:Smoking Cessation / Q000379:methods*; D057968:Transdermal Patch
D018759:Adrenergic Uptake Inhibitors; D000929:Antidepressive Agents, Tricyclic; D048271:Chitosan; D009661:Nortriptyline