Computer-based formulation design and optimization using Hansen solubility parameters to enhance the delivery of ibuprofen through the skin

The effect of alcohols as vehicles on the percutaneous absorption and skin retention of ibuprofen modified with l-valine alkyl esters

“…50,51 In vitro penetration of ibuprofen through porcine skin has previously been evaluated in many studies. 17,[52][53][54][55] Higher penetration of IBU derivatives through pig skin is conrmed by Furukawa et al, where ibuprofen-ProOEt permeated ten-times higher than for free ibuprofen and variation in skin permeation depends on strong ion-pairing between a cation and an anionic drug. 37 In our in vitro study, the penetration of new ibuprofen derivatives was compared with the penetration of parent ibuprofen.…”

Evaluation of Formulation Parameters on Permeation of Ibuprofen from Topical Formulations Using Strat-M® Membrane

“…Addition of mucoadhesive agents in the formulation could have resulted in increased retention, prolonged contact, and reduced leakage of formulation and thus increasing the permeation. Additionally, these agents increase level of hydration in the membrane interface which in turn decreases the diffusional path length and thus favoring the transport of ibuprofen [24,41]. In addition, mucoadhesive agents could have increased the concentration gradient due to prolonged contact of the formulation at the membrane interface and resulting in enhanced permeation [42,43].…”

“…It is reported in the literature that emulgels provide better solubility for poorly water-soluble drugs like ibuprofen and enhance the skin permeability. Higher permeation of ibuprofen with emulgels compared to creams could be attributed to increased thermodynamic activity of ibuprofen, due to a change in the vehicle where ibuprofen was more soluble, or due to a different interaction of the formulation with the membrane [24,49,50].…”

“…In general, there is a lack of scientific evaluation on how the formulation properties, such as concentration of drug, physical state of the drug, and formulation type, influence the bioavailability of conventional topical dosage forms, such as creams and gels. Although several studies have evaluated the effect of formulation properties on transdermal permeation of drugs, the scientific data show that the research was limited to only one factor, such as concentration of drug [22], concentration of excipients [7,23], and formulation type [24,25]. Therefore, the current study was designed to provide ready information to the formulators who design and develop topical semisolid formulations on the impact of formulation properties (concentration of drug, physical state of the drug, mucoadhesive agents, and formulation type) on transdermal permeation.…”

“…Although, NSAIDs are very effective, their oral absorption is associated with severe gastric irritation leading to gastric bleeding and ulcers. Therefore, topical/transdermal delivery of NSAIDs is preferred as it bypasses hepatic first pass metabolism and also results in targeted effect at the site of inflammation/pain [24]. Majority of the NSAIDs (salicylates, acetic acid derivatives, enol acid derivatives, and propionic acid derivatives) approved by USFDA have similar physicochemical properties (molecular mass, logP, and pK a ) [27][28][29][30].…”