Polymeric Matrix System for Prolonged Delivery of Tramadol Hydrochloride, Part II: Biological Evaluation

Abstract

Abstract. This study is an extrapolation of our previous one (part I) concerned with the formulation and physicochemical evaluation of a novel, simple, monolayer, easy-to-use, cost-effective, and aesthetically acceptable bioadhesive transdermal patch for tramadol hydrochloride. The current work is focused on bioadhesion, skin tolerability, and pharmacodynamic evaluation. Using naked rat skin, chitosanEudragit® NE30D (1:1) film attained best bioadhesive properties. During in vivo studies, it also showed a significantly extended analgesic effect compared to both oral formula and chitosan single polymeric film using the hot plate test method. All the polymeric films were skin tolerable for the intended period of application according to the Draize test. The success of our approach can proudly, positively contribute into the world of pain management and arguably push transdermal delivery to realize its great promise.

In-vitro and in-vivo transdermal iontophoretic delivery of tramadol, a centrally acting analgesic

“…When the anodal iontophoretic patch system was applied in combination with a constant current supply (250 µA/cm 2 ) for 6 h on the abdominal skin of conscious guinea pig, both plasma concentrations and in‐vivo transdermal absorption rate of tramadol reached a peak 3 h after the initiation of current supply and were sustained for the subsequent 3 h. This result indicates that the transdermal input rate of tramadol was in equilibrium with its elimination rate and the steady‐state plasma concentration of tramadol was maintained under constant current supply. In contrast to the present result, a passive‐type transdermal delivery system of tramadol using a polymeric matrix was reported not to sustain stable efficacy after reaching the peak effect, but nevertheless to provide prolonged efficacy compared with oral administration in rats [12] . One of advantages of iontophoretic transdermal drug delivery over passive transdermal delivery is the maintenance of stable blood concentrations of drugs and therefore efficacy as a result of controlling the transdermal transport of permeates based on the amount of applied current [8,12,16,18] .…”

“…Transdermal drug delivery, a non‐invasive drug administration route, offers the potential benefits of simplicity, efficacy and patient acceptance by maintaining a constant blood drug concentration for an extended period of time with acceptable interpatient variations [6–8] . In addition, the transdermal delivery system can decrease the possible abuse and addiction potential of tramadol [9,10] by avoiding peak and trough plasma concentrations and by reducing the total amount of medication input [11,12] . Hence, a transdermal delivery system is a desirable alternative administration route for tramadol hydrochloride for patients with chronic pain.…”

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

“…However, the ex vivo permeation studies provide a valuable insight on the in vivo performance of many products (Ammar et al, 2009). The rectum is known to have a similar epithelium to that of the upper GI tract and the predominant mechanism of permeation through the rectal mucosa appears to involve transcellular passage across the cell membrane (Kamel et al, 2013).…”

Topical Nanoemmigel Formulation of Boswellia serrata

“…A single dose of formulation was applied on the left side of the rat, with the right side as control. The development of erythema was monitored after 24 h and 14 d [18][19][20] .…”