Bot Detector
IJPC Seal
Download FREE Sample Issue or Article
LEARN MORE
Subscribe Today
A subscription to IJPC provides on-line access to full-text, full-color, printable PDF copies of all issues and individual articles published by the Journal since 1997.

Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel

Author(s):  Woodall Rachel, Arnold John J, McKay Doug, Abill C Scott

Issue:  May/Jun 2013 - Volume 17, Number 3
View All Articles in Issue

Page(s):  247-253

Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel Page 1
Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel Page 2
Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel Page 3
Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel Page 4
Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel Page 5
Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel Page 6
Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel Page 7

Download in electronic PDF format for $75

Abstract:  The purpose of this study was to assess the impact of altering formulation pH on the transdermal penetration of several commonly used antiemetic, weakly basic drugs incorporated into poloxamer lecithin organogel vehicle. Poloxamer lecithin organogel formulations containing promethazine hydrochloride (25 mg/mL), metoclopramide hydrochloride (10 mg/mL), and ondansetron hydrochloride (8 mg/mL) were examined for both drug release and transdermal penetration across porcine skin in modified Franz diffusion cells for a period of 24 hours. For the transdermal studies, each antiemetic drug was formulated at a pH above and below their acid dissociation constant (pKa) in an attempt to assure that the drug would be primarily in their respective ionized or non-ionized states. In addition, drug content in skin was assessed at the end of the 24-hour experiment. Drug content analysis was determined via high-performance liquid chromatography. As a percent of total drug release from the poloxamer lecithin organogel vehicle, promethazine hydrochloride demonstrated the most transdermal drug penetration after 24 hours (30.2% ± 20.2%), followed by ondansetron hydrochloride (2.7% ± 1.1%) and metoclopramide hydrochloride (1.8% ± 1.6%). Subsequently, the pH of the Pluronic F-127 gel was adjusted in order to ensure that each antiemetic drug would be primarily in its unionized state. The transdermal permeation of each antiemetic drug primarily in its unionized state increased over that observed with the drug primarily in its ionized state after 24 hours (promethazine: 1.6-fold increase; metoclopramide: 1.3-fold increase; ondansetron: 1.8-fold increase). A similar trend was noted in the amount of each drug found in the skin after 24 hours (promethazine: 1.2-fold increase; metoclopramide: 2.4-fold increase; ondansetron: 3.0-fold increase). These results suggest that proper optimization of drug ionization state may be a useful strategy for compounding pharmacists to increase the efficacy of drugs intended for inclusion in transdermal formulations.

Related Keywords: formulations, formulation pH, drug ionization state, transdermal penetration, skin absorption, antiemetic agents, nausea, vomiting, poloxamer lecithin organogel, pluronic lecithin organogel, PLO, topical preparation, promethazine hydrochloride, metoclopramide hydrochloride, ondansetron hydrochloride, high-performance liquid chromatograph, HPLC, drug release

Related Categories: EXCIPIENTS, FORMULATIONS, PEER-REVIEWED, DOSAGE FORMS/DRUG CARRIERS

Printer-Friendly Version



Related Articles from IJPC
Title/Author
(Click for Abstract / Details / Purchase)
Issue/​Page
View/Buy
Effect of Formulation pH on Transdermal Penetration of Antiemetics Formulated in Poloxamer Lecithin Organogel
Woodall Rachel
, Arnold John J, McKay Doug, Abill C Scott
May/Jun 2013
Pg. 247-253

Veterinary Transdermal Medications: A to Z
Davidson Gigi S
Mar/Apr 2003
Pg. 106-113

The Release and Transdermal Penetration of Baclofen Formulated in a Poloxamer Lecithin Organogel
Arnold John J
, Asbill Scott
Nov/Dec 2009
Pg. 569-571

Skin Penetration and Antinociception of Topical Gabapentin Formulations
Bryson Evan
, Asbill Scott, Sweitzer Sarah
Nov/Dec 2014
Pg. 504-511

In Vitro Skin Penetration and Skin Content of Progesterone from Various Topical Formulations
Heustess Allie
, Asbill Scott, Eagerton David, Arnold John
Nov/Dec 2014
Pg. 512-515

Wetting and/or Solubilizing Agents, Featured Excipient:
Allen Loyd V Jr
Jul/Aug 2001
Pg. 310-312

Preparation and In Vitro Evaluation of a Pluronic Lecithin Organogel Containing Ricinoleic Acid for Transdermal Delivery
Boddu Sai HS
, Bonam Sindhu Prabha, Wei Yangjie, Alexander Kenneth
May/Jun 2014
Pg. 256-261

Feline Transdermal Formulation Considerations
Forsythe Lauren Eichstadt
Nov/Dec 2017
Pg. 446-452

Gabapentin in Elastic Liposomes: Preparation, Characterization, Drug Release, and Penetration Through Porcine Skin
Le Uyen Minh
, Baltzley Sarah, AlGhananeem Abeer
Nov/Dec 2018
Pg. 498-503

The Use of Pluronic Lecithin Organogels in the Transdermal Delivery of Drugs
Bramwell Bethany L
, Williams LaVonn A
Jan/Feb 2012
Pg. 62-63

Effect of Penetration Enhancers on the Percuaneous Delivery of Hormone Replacement Actives
Trimble John O
, Light Bob
Nov/Dec 2017
Pg. 530-535

Enhancement of Skin Penetration of Nonsteroidal Anti-Inflammatory Drugs from Extemporaneously Compounded Topical-Gel Formulations
Goodwin Donald A
, Fuhram L Clifton
Nov/Dec 1999
Pg. 496-500

Effect of Penetration Enhancers on the Percutaneous Delivery of Pain Management Actives
Trimble John
, Light Bob
May/Jun 2016
Pg. 250-256

Percutaneous Absorption of Lorazepam, Diphenhydramine Hydrochloride, and Haloperidol from ABH Gel
Dahal Amit
, Neupane Rabin, Boddu Sai HS, Renukuntla Jwala, Khupse Rahul, Dudley Richard
Mar/Apr 2020
Pg. 168-175

Evaluation of Compounded Transdermal Analgesic Formulations Using the Franz Finite Dose Model
Baneshi Marzieh
, Tyagi Deependra, Panneerselvam Ezilrani, MacKenzie Graham, Coleman Johngary, Zhang Shine X
Sep/Oct 2023
Pg. 424-430

Transdermals: The Skin as Part of a Drug Delivery System
Allen Loyd V Jr
Jul/Aug 2011
Pg. 308-315

Promethazine 25 mg/mL in Pluronic Lecithin Organogel for Nausea and Vomiting in a Pediatric Patient: A Case Report
Muller George
May/Jun 2009
Pg. 220-221

Bioavailability of Promethazine in a Topical Pluronic Lecithin Organogel: A Pilot Study
Glisson James K
, Wood Rebecca L, Kyle Patrick B, Cleary John D
May/Jun 2005
Pg. 242-246

Stability of Methimazole in Poloxamer Lecithin Organogel to Determine Beyond-Use Date
Pignato Alyssa
, Pankaskie Marvin, Birnie Christine
Nov/Dec 2010
Pg. 522-525

Poloxamers, Featured Excipient:
Allen Loyd V Jr
Jan/Feb 2002
Pg. 58-59

Return to Top