Abstract
Topical drug delivery is an attractive alternative to conventional methods because of advantages such as non-invasive delivery, by-pass of first pass metabolism, and improved patient compliance. However, several factors such as skin, physicochemical properties of the drug, and vehicle characteristics influence the permeation. Within a formulation, critical factors such as concentration of drug, physical state of drug in the formulation, and organoleptic properties affect the flux across the skin. The aim of the study was to develop and investigate topical semisolid preparations (creams and gels) with ibuprofen as the model drug and investigate the effect of various formulation parameters on the in-vitro performance across the Strat-M® membrane using flow-through cells. In addition, the physical stability of the developed formulations was investigated by studying viscosity, pH, and appearance. All the formulations developed in the study had appealing appearance with smooth texture and no signs of separation. Viscosity and pH of the formulations were acceptable. Cumulative amount of drug permeated at the end of 24 h was highest for clear gel (3% w/w ibuprofen; F6: 739.6 ± 36.1 µg/cm2) followed by cream with high concentration of ibuprofen in suspended form (5% w/w; F3: 320.8 ± 17.53 µg/cm2), emulgel (3% w/w ibuprofen; F5: 178.5 ± 34.5 µg/cm2), and cream with solubilized ibuprofen (3% w/w; F2A: 163.2 ± 9.36 µg/cm2). Results from this study showed that permeation of ibuprofen was significantly influenced by formulation parameters such as concentration of ibuprofen (3% vs. 5% w/w), physical state of ibuprofen (solubilized vs. suspended), formulation type (cream vs. gel), mucoadhesive agents, and viscosity (high vs. low). Thus, findings from this study indicate that pharmaceutical formulation scientists should explore these critical factors during the early development of any new topical drug product in order to meet pre-determined quality target product profile.
Highlights
Topical/transdermal drug delivery refers to the delivery of drugs via skin and is an attractive alternative to conventional methods such as oral and parenteral routes
It is already known that active drug accounts only for a minor fraction in the formulation and; it is important to Formulation of a topical drug product for lipophilic drugs with desirable Quality Target Product Profile (QTPP) is challenging
The aim of the present study was to investigate the effect of formulation parameters, such as concentration of drug, physical state of the drug, addition of mucoadhesive agents, and formulation type, on permeation of ibuprofen from semisolid formulations
Summary
Topical/transdermal drug delivery refers to the delivery of drugs via skin and is an attractive alternative to conventional methods such as oral and parenteral routes. Several other factors such as physicochemical properties of the drug (lipophilicity, solubility, molecular weight or size, and hydrogen bonding) and characteristics of a formulation/vehicle or a drug delivery system influence the permeation [7] To overcome these challenges, several physical and chemical methods have been employed to enhance the transport of drugs through the skin. In addition to penetration enhancers, several other excipients/additives such as solvents, co-solvents, surfactants, humectants, thickening agents, and others are used in the development of topical/transdermal formulation These agents act as inactive ingredients and control the extent of absorption (thermodynamic activity and partition coefficient), maintain the viscosity and pH, improve the stability as well as organoleptic properties, and increase the bulk of the formulation [15,16]. In case of topical product development, achieving the target flux is a challenge as it is dependent of several factors
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