An Investigation into the Influence of Counterion on the RS‐Propranolol and S‐Propranolol Skin Permeability

Cilurzo, Francesco; Minghetti, Paola; Alberti, Elisabetta; Gennari, C.; Pallavicini, Marco; Valoti, Ermanno; Montanari, L.

doi:10.1002/jps.21891

Cited by 14 publications

(19 citation statements)

References 13 publications

(15 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As shown in table 4, sodium methylparaben in solution induced a shift of pH to a value near the pK a of PR (9.5 ± 1.2) [21]. In line with the Henderson-Hasselbalch equation, the inner pH of the aqueous phase of the semi-solid formulation modifies the ionization equilibrium of PR-Cl and the PR-free base, which penetrates easily through the human epidermis [13]. In particular, when the pH is near the pK a of PR, the concentration of free base increases, inducing an increase in the permeation flux due to more appropriate physicochemical characteristics for the absorption process.…”

Section: Discussionmentioning

confidence: 91%

“…As a matter of fact, the semi-solid vehicle itself is able to influence in many ways the permeation of molecules through the human epidermis [15,16]. In addition to a direct effect on the drug concentration gradient, characteristics of semi-solid bases impact indirectly on K SC/W and D SCE , inducing modifications in the inner structure of the stratum corneum [13,26]. For example, the higher in vivo performance of lipophilic creams in comparison to the observed in vitro pattern could be due to the enhancement of drug permeation related to the occlusive properties of the semi-solid matrix [17,26].…”

Section: Discussionmentioning

confidence: 99%

“…In general, drug permeation through the human epidermis is a passive diffusion process that depends on both the physicochemical properties of the drug (e.g., molecular weight, log P) and vehicle. In the case of PR, several studies have demonstrated a good permeation profile through human skin, but this process is strongly related to its ionization rate and the type of counter ions [13,14]. On the other hand, the composition of the semi-solid vehicle is also critical because it strongly influences the drug physicochemical stability and its release and permeation profiles [15,16,17].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Casiraghi

Musazzi²,

Rocco³

et al. 2016

Skin Pharmacol Physiol

Self Cite

View full text Add to dashboard Cite

Background/Aim: Topical β-blockers have recently been proposed as a valid alternative to oral drugs for treating cutaneous infantile haemangiomas, but clinical results in the literature are inconsistent due to the empirical choice of topical preparations. The current investigation aimed to rationalize the selection of a semi-solid vehicle for a locally applied drug product containing 1% w/w propranolol hydrochloride (PR-Cl). Methods: A hydrophobic ointment of PR-Cl, two lipophilic creams, and a hydrophilic cream were prepared. In vitro release and skin permeation studies through human epidermis and full-thickness skin were performed by Franz diffusion cells. Results: The overall results highlighted that PR-Cl was able to permeate the human epidermis, and its penetration pattern was strongly influenced by the composition of the semi-solid vehicle. PR-Cl release and permeation from lipophilic vehicles were extremely limited and influenced by their composition. Best results were obtained by using the hydrophilic cream. Furthermore, the retention study evidenced that epidermis acted as a reservoir, releasing the PR-Cl accumulated after preparation removal. Conclusion: The 1% w/w PR-Cl cream resulted the most suitable formulation for improving drug permeation through the human epidermis. On the contrary, the negligible permeation profile through full-thickness skin pointed out that PR-Cl cannot diffuse significantly to reach the deeper layers of human skin.

show abstract

Section: Discussionmentioning

confidence: 91%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Casiraghi

Musazzi²,

Rocco³

et al. 2016

Skin Pharmacol Physiol

Self Cite

View full text Add to dashboard Cite

show abstract

“…The in vitro skin permeability of PR hydrochloride through human skin was reported in several papers 2 . It was also demonstrated that the skin permeation of the unionized form was higher than the corresponding salts 3 . Nevertheless, the only available pharmacokinetic data were referred to films made of poly(methyl methacrylate) 4 or cellulose ethers 5 .…”

Section: Introductionmentioning

confidence: 97%

Formulation study of a patch containing propranolol by design of experiments

Cilurzo

Minghetti

Casiraghi

et al. 2013

Drug Development and Industrial Pharmacy

Self Cite

View full text Add to dashboard Cite

show abstract

“…The membrane composition was optimized reducing the number of components in order to simplify its preparation and favour the reproducibility. The membrane performances were tested using three model molecules chosen on the basis of their different diffusion and solubility properties: (RS)-ibuprofen [19], (RS)-propranolol [20] and testosterone [1]. The drug permeation amounts were compared to those obtained in a set of experiments carried out using human epidermis as membrane [1,2].…”

Section: Introductionmentioning

confidence: 99%

Regenerated keratin membrane to match the in vitro drug diffusion through human epidermis

Selmin

Cilurzo

Aluigi

et al. 2012

Results in Pharma Sciences

Self Cite

View full text Add to dashboard Cite

This work aimed to develop membranes made of regenerated keratin and ceramides (CERs) to match the barrier property of the human stratum corneum in in vitro percutaneous absorption studies. The membrane composition was optimized on the basis of the in vitro drug diffusion profiles of ibuprofen, propranolol and testosterone chosen as model drugs on the basis of their different diffusion and solubility properties. The data were compared to those obtained using human epidermis.The ATR-FTIR and SEM analyses revealed that CERs were suspended into the regenerated keratin matrix, even if a partial solubilization occurred. It resulted in the membranes being physically stable after exposure to aqueous buffer and/or mineral oil and the fluxes of ibuprofen and propranolol from these vehicles through membranes and human skin were of the same order of magnitude. The best relationship with human epidermis data was obtained with 180 μm-thick membrane containing 1% ceramide III and 1% ceramide VI. The data on the testosterone diffusion were affected by the exposure of the membrane to a water/ethanol solution over a prolonged period of time, indicating that such an organic solvent was able to modify the supermolecular organization of keratin and CERs.The keratin/CER membranes can represent a simplified model to assay the in vitro skin permeability study of small molecules.

show abstract

An Investigation into the Influence of Counterion on the RS‐Propranolol and S‐Propranolol Skin Permeability

Cited by 14 publications

References 13 publications

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Formulation study of a patch containing propranolol by design of experiments

Regenerated keratin membrane to match the in vitro drug diffusion through human epidermis

Contact Info

Product

Resources

About