scholarly journals Preparation, Characterization and Dermal Delivery of Methadone

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 509 ◽  
Author(s):  
Chin-Ping Kung ◽  
Bruno C. Sil ◽  
Jonathan Hadgraft ◽  
Majella E. Lane ◽  
Bhumik Patel ◽  
...  
Keyword(s):  
Ethyl Oleate ◽  
Dosage Forms ◽  
Attractive Alternative ◽  
Free Base ◽  
Porcine Skin ◽  
Promising Candidate ◽  
In Vitro Permeation ◽  
Dermal Delivery ◽  
Future Work

The use of methadone for the management of pain has received great interest in recent years. Currently, oral and intravenous formulations are available for clinical use. Dermal delivery represents an attractive alternative route of administration for this drug as it is associated with comparatively fewer side effects. The first stage of the work was the preparation of methadone free base as this form of the drug is expected to permeate the skin to a greater extent than the hydrochloride salt. Subsequently the molecule was characterized with Nuclear Magnetic Resonance (NMR) and thermal analysis, the distribution coefficient was determined and solubility studies were conducted in a range of solvents. In vitro permeation and mass balance studies were conducted under finite dose conditions (5 μL/cm2) in porcine skin. The results confirmed the more favorable penetration of methadone free base compared with the salt. The highest cumulative amount of methadone (41 ± 5 μg/cm2) permeated from d-limonene (LIM). Ethyl oleate (EO), Transcutol® P (TC) and octyl salicylate (OSAL) also appear to be promising candidate components of dermal formulations for methadone base. Future work will focus on further formulation optimization with the objective of progressing to evaluation of prototype dosage forms in clinical trials.

scholarly journals Dermal delivery of amitriptyline for topical analgesia

2021 ◽  
Author(s):  
Chin-Ping Kung ◽  
Bruno C. Sil ◽  
Yanling Zhang ◽  
Jonathan Hadgraft ◽  
Majella E. Lane ◽  
...  
Keyword(s):  
Treatment Options ◽  
Isopropyl Myristate ◽  
Promising Candidate ◽  
In Vitro Permeation ◽  
Base Form ◽  
Dermal Delivery ◽  
Phosphate Buffered Saline ◽  
Topical Analgesia ◽  
Topical Analgesic

Abstract Amitriptyline, administered orally, is currently one of the treatment options for the management of neuropathic pain and migraine. Because of the physicochemical properties of the molecule, amitriptyline is also a promising candidate for delivery as a topical analgesic. Here we report the dermal delivery of amitriptyline from a range of simple formulations. The first stage of the work required the conversion of amitriptyline hydrochloride to the free base form as confirmed by nuclear magnetic resonance (NMR). Distribution coefficient values were measured at pH 6, 6.5, 7, and 7.4. Solubility and stability of amitriptyline were assessed prior to conducting in vitro permeation and mass balance studies. The compound demonstrated instability in phosphate-buffered saline (PBS) dependent on pH. Volatile formulations comprising of isopropyl alcohol (IPA) and isopropyl myristate (IPM) or propylene glycol (PG) were evaluated in porcine skin under finite dose conditions. Compared with neat IPM, the IPM:IPA vehicles promoted 8-fold and 5-fold increases in the amount of amitriptyline that permeated at 24 h. Formulations containing PG also appear to be promising vehicles for dermal delivery of amitriptyline, typically delivering higher amounts of amitriptyline than the IPM:IPA vehicles. The results reported here suggest that further optimization of topical amitriptyline formulations should be pursued towards development of a product for clinical investigational studies. Graphical abstract

scholarly journals Preparation, Characterisation, and Topical Delivery of Terbinafine

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 548 ◽  
Author(s):  
A. S. M. Monjur Al Hossain ◽  
Bruno C. Sil ◽  
Fotis Iliopoulos ◽  
Rebecca Lever ◽  
Jonathan Hadgraft ◽  
...  
Keyword(s):  
Propylene Glycol ◽  
Fungal Infections ◽  
Isopropyl Myristate ◽  
Limited Information ◽  
Free Base ◽  
Porcine Skin ◽  
Salt Form ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 200

Terbinafine (TBF) is commonly used in the management of fungal infections of the skin because of its broad spectrum of activity. Currently, formulations containing the free base and salt form are available. However, there is only limited information in the literature about the physicochemical properties of this drug and its uptake by the skin. In this work, we conducted a comprehensive characterisation of TBF, and we also examined its percutaneous absorption in vitro in porcine skin. TBF-free base was synthesised from the hydrochloride salt by a simple proton displacement reaction. Both the free base and salt form were further analysed using Differential Scanning Calorimetry (DSC) and Thermogravimetric Analysis (TGA). Delivery of TBF-free base in excised porcine skin was investigated from the following solvents: Isopropyl myristate (IPM), propylene glycol monolaurate (PGML), Transcutol® (TC), propylene glycol (PG), polyethylene glycol 200 (PEG 200), oleic acid (OL), ethanol (EtOH), and isopropyl alcohol (IPA). Permeation and mass balance studies confirmed that PG and TC were the most efficacious vehicles, delivering higher amounts of TBF-free base to the skin compared with a commercial gel (p < 0.05). These preliminary results are promising and will inform the development of more complex formulations in future work.

scholarly journals An Investigation of the Influence of PEG 400 and PEG-6-Caprylic/Capric Glycerides on Dermal Delivery of Niacinamide

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2907
Author(s):  
Yanling Zhang ◽  
Majella E. Lane ◽  
David J. Moore
Keyword(s):  
Skin Permeation ◽  
Ternary Systems ◽  
Pharmaceutical Products ◽  
Porcine Skin ◽  
Peg 400 ◽  
Skin Delivery ◽  
Dermal Delivery ◽  
Binary And Ternary Systems ◽  
Skin Retention

Polyethylene glycols (PEGs) and PEG derivatives are used in a range of cosmetic and pharmaceutical products. However, few studies have investigated the influence of PEGs and their related derivatives on skin permeation, especially when combined with other solvents. Previously, we reported niacinamide (NIA) skin permeation from a range of neat solvents including propylene glycol (PG), Transcutol® P (TC), dimethyl isosorbide (DMI), PEG 400 and PEG 600. In the present work, binary and ternary systems composed of PEGs or PEG derivatives combined with other solvents were investigated for skin delivery of NIA. In vitro finite dose studies were conducted (5 μL/cm2) in porcine skin over 24 h. Higher skin permeation of NIA was observed for all vehicles compared to PEG 400. However, overall permeation for the binary and ternary systems was comparatively low compared with results for PG, TC and DMI. Interestingly, values for percentage skin retention of NIA for PEG 400:DMI and PEG 400:TC were significantly higher than values for DMI, TC and PG (p < 0.05). The findings suggest that PEG 400 may be a useful component of formulations for the delivery of actives to the skin rather than through the skin. Future studies will expand the range of vehicles investigated and also look at skin absorption and residence time of PEG 400 compared to other solvents.

scholarly journals Novel Design Approaches in the Fabrication of Polymeric Microarray Patches via Micromoulding

Micromachines ◽  
2020 ◽  
Vol 11 (6) ◽  
pp. 554 ◽  
Author(s):  
Inken Ramöller ◽  
Emma McAlister ◽  
Abigail Bogan ◽  
Ana Cordeiro ◽  
Ryan Donnelly
Keyword(s):  
Skin Barrier ◽  
Systemic Delivery ◽  
Porcine Skin ◽  
Density Maps ◽  
In Vitro Permeation ◽  
Wide Range ◽  
Significant Difference ◽  
Permeation Studies ◽  
Novel Design

The focus on novel systems for transdermal delivery of therapeutic agents has increased considerably over recent years, as this administration route comes with many advantages. Polymeric microarray patches (MAPs) are minimally invasive devices that enable systemic delivery of a wide range of drugs by overcoming the outer skin barrier. Conventionally, MAPs fabricated by micromoulding have a low needle density. In this study, the performance of hydrogel-forming MAPs cast using novel industrially manufactured micromoulds with a high needle density (600 needles/0.75 cm2) was compared to that of MAPs obtained using conventional moulds with a lower density (196 needles/0.89 cm2). Surrounding holders for micromoulds were designed for time-efficient fabrication of MAPs. The influence of needle densities on mechanical strength, insertion efficiency and in vitro permeation of ibuprofen sodium (IBU) was analysed. Insertion of both MAPs into an artificial skin model and neonatal porcine skin was comparable. No significant difference was observed in permeation studies of IBU (p > 0.05), with a delivery of 8.7 ± 1.7 mg for low-density and 9.5 ± 0.1 mg for high-density MAPs within 24 h. This highlights the potential of these novel micromoulds for manufacturing polymeric MAPs with a higher needle density for future applications.

scholarly journals In vitro permeation and disposition of niacinamide in silicone and porcine skin of skin barrier-mimetic formulations

2017 ◽  
Vol 520 (1-2) ◽  
pp. 158-162 ◽  
Author(s):  
Tasnuva Haque ◽  
Majella E. Lane ◽  
Bruno C. Sil ◽  
Jonathan M. Crowther ◽  
David J. Moore
Keyword(s):  
Skin Barrier ◽  
Porcine Skin ◽  
In Vitro Permeation

Formulation and Evaluation of Carbopol Gel Containing Liposomes of Ketoconazole. (Part-II)

2009 ◽  
Vol 1 (2) ◽  
Author(s):  
Rakesh Patel ◽  
Hardik Patel ◽  
Ashok Baria
Keyword(s):  
Antifungal Activity ◽  
Rat Skin ◽  
Albino Rat ◽  
In Vitro Drug Release ◽  
Carbopol Gel ◽  
Liposomal Formulations ◽  
Release Drug ◽  
In Vitro Permeation ◽  
In Vitro Antifungal Activity

The aim of this work was to prepare and evaluate the topical carbopol gel formulation containing ketoconazole encapsulated liposomes. Ketoconazole loaded liposomes were prepared by thin film hydration technique. The prepared liposomes were incorporated into 1% carbopol gel, and the systems were evaluated for in-vitro drug release, drug retention into skin and in-vitro antifungal activity. The in-vitro permeation of ketoconazole using wistar albino rat skin from liposomal gel was compared with that of plain drug gel and also with plain drug cream containing 2% w/w of ketoconazole. The release of ketoconazole from liposomal gel was much slower than from non liposomal formulations. Gel containing liposomal ketoconazole showed maximum antifungal activity after 30 hours over plain ketoconazole gel and cream formulations.

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