Preparation and the Biopharmaceutical Evaluation for the Metered Dose Transdermal Spray of Dexketoprofen

Overview

Journal J Drug Deliv

Date 2014 Mar 25

PMID 24660066

Citations 6

Authors

Wangding Lu

Huafei Luo

Zhuangzhi Zhu

Yubo Wu

Jing Luo

Hao Wang

Affiliations

Soon will be listed here.

Abstract

The objective of the present work was to develop a metered dose transdermal spray (MDTS) formulation for transdermal delivery of dexketoprofen (DE). DE release from a series of formulations was assessed in vitro. Various qualitative and quantitative parameters like spray pattern, pump seal efficiency test, average weight per metered dose, and dose uniformity were evaluated. The optimized formulation with good skin permeation and an appropriate drug concentration and permeation enhancer (PE) content was developed incorporating 7% (w/w, %) DE, 7% (v/v, %) isopropyl myristate (IPM), and 93% (v/v, %) ethanol. In vivo pharmacokinetic study indicated that the optimized formulation showed a more sustainable plasma-concentration profile compared with the Fenli group. The antiinflammatory effect of DE MDTS was evaluated by experiments involving egg-albumin-induced paw edema in rats and xylene-induced ear swelling in mice. Acetic acid-induced abdominal constriction was used to evaluate the anti-nociceptive actions of DE MDTS. Pharmacodynamic studies indicated that the DE MDTS has good anti-inflammatory and anti-nociceptive activities. Besides, skin irritation studies were performed using rat as an animal model. The results obtained show that the MDTS can be a promising and innovative therapeutic system used in transdermal drug delivery for DE.

Citing Articles

A Comprehensive Review of the Strategies to Reduce Retinoid-Induced Skin Irritation in Topical Formulation.

Narsa A, Suhandi C, Afidika J, Ghaliya S, Elamin K, Wathoni N Dermatol Res Pract. 2024; 2024:5551774.

PMID: 39184919 PMC: 11344648. DOI: 10.1155/2024/5551774.

Film-Forming Sprays for Topical Drug Delivery.

Umar A, Butarbutar M, Sriwidodo S, Wathoni N Drug Des Devel Ther. 2020; 14:2909-2925.

PMID: 32884234 PMC: 7434377. DOI: 10.2147/DDDT.S256666.

Functional Fragments of AIMP1-Derived Peptide (AdP) and Optimized Hydrosol for Their Topical Deposition by Box-Behnken Design.

Lee J, Han Y, Kwon T, Kim D, Lee H, Jung W Molecules. 2019; 24(10).

PMID: 31121831 PMC: 6572189. DOI: 10.3390/molecules24101967.

Medicated Foams and Film Forming Dosage Forms as Tools to Improve the Thermodynamic Activity of Drugs to be Administered Through the Skin.

Gennari C, Selmin F, Minghetti P, Cilurzo F Curr Drug Deliv. 2019; 16(5):461-471.

PMID: 30657040 PMC: 6637090. DOI: 10.2174/1567201816666190118124439.

Transdermal Evaporation Drug Delivery System: Concept to Commercial Products.

Parhi R, Swain S Adv Pharm Bull. 2019; 8(4):535-550.

PMID: 30607327 PMC: 6311647. DOI: 10.15171/apb.2018.063.

References

Dick I, Scott R . Pig ear skin as an in-vitro model for human skin permeability. J Pharm Pharmacol. 1992; 44(8):640-5. DOI: 10.1111/j.2042-7158.1992.tb05485.x. View

Raghavan S, Trividic A, Davis A, Hadgraft J . Effect of cellulose polymers on supersaturation and in vitro membrane transport of hydrocortisone acetate. Int J Pharm. 1999; 193(2):231-7. DOI: 10.1016/s0378-5173(99)00345-2. View

Landoni M, Lees P . Pharmacokinetics and pharmacodynamics of ketoprofen enantiomers in calves. Chirality. 1995; 7(8):586-97. DOI: 10.1002/chir.530070806. View

Oliveira G, Hadgraft J, Lane M . The influence of volatile solvents on transport across model membranes and human skin. Int J Pharm. 2012; 435(1):38-49. DOI: 10.1016/j.ijpharm.2012.05.037. View

Landoni M, Comas W, Mucci N, Anglarilli G, Bidal D, Lees P . Enantiospecific pharmacokinetics and pharmacodynamics of ketoprofen in sheep. J Vet Pharmacol Ther. 2000; 22(6):349-59. DOI: 10.1046/j.1365-2885.1999.00209.x. View

Gooren L, Bunck M . Transdermal testosterone delivery: testosterone patch and gel. World J Urol. 2003; 21(5):316-9. DOI: 10.1007/s00345-003-0368-6. View

Zhou M, Wang H, Suolangjiba , Kou J, Yu B . Antinociceptive and anti-inflammatory activities of Aquilaria sinensis (Lour.) Gilg. Leaves extract. J Ethnopharmacol. 2008; 117(2):345-50. DOI: 10.1016/j.jep.2008.02.005. View

Thomas B, Finnin B . The transdermal revolution. Drug Discov Today. 2004; 9(16):697-703. DOI: 10.1016/S1359-6446(04)03180-0. View

Leichtnam M, Rolland H, Wuthrich P, Guy R . Formulation and evaluation of a testosterone transdermal spray. J Pharm Sci. 2006; 95(8):1693-702. DOI: 10.1002/jps.20641. View

10.

Jacobi U, Kaiser M, Toll R, Mangelsdorf S, Audring H, Otberg N . Porcine ear skin: an in vitro model for human skin. Skin Res Technol. 2007; 13(1):19-24. DOI: 10.1111/j.1600-0846.2006.00179.x. View

11.

Oliveira G, Beezer A, Hadgraft J, Lane M . Alcohol enhanced permeation in model membranes. Part I. Thermodynamic and kinetic analyses of membrane permeation. Int J Pharm. 2010; 393(1-2):61-7. DOI: 10.1016/j.ijpharm.2010.03.062. View

12.

Bakshi A, Bajaj A, Malhotra G, Madan M, Amrutiya N . A novel metered dose transdermal spray formulation for oxybutynin. Indian J Pharm Sci. 2011; 70(6):733-9. PMC: 3040866. DOI: 10.4103/0250-474X.49094. View

13.

Trottet L, Merly C, Mirza M, Hadgraft J, Davis A . Effect of finite doses of propylene glycol on enhancement of in vitro percutaneous permeation of loperamide hydrochloride. Int J Pharm. 2004; 274(1-2):213-9. DOI: 10.1016/j.ijpharm.2004.01.013. View

14.

Zurdo Schroeder I, Franke P, Schaefer U, Lehr C . Development and characterization of film forming polymeric solutions for skin drug delivery. Eur J Pharm Biopharm. 2006; 65(1):111-21. DOI: 10.1016/j.ejpb.2006.07.015. View

15.

Herwadkar A, Sachdeva V, Taylor L, Silver H, Banga A . Low frequency sonophoresis mediated transdermal and intradermal delivery of ketoprofen. Int J Pharm. 2011; 423(2):289-96. DOI: 10.1016/j.ijpharm.2011.11.041. View

16.

Stinchcomb A, Pirot F, Touraille G, Bunge A, Guy R . Chemical uptake into human stratum corneum in vivo from volatile and non-volatile solvents. Pharm Res. 1999; 16(8):1288-93. DOI: 10.1023/a:1014866001386. View

17.

Aberg G, Ciofalo V, Pendleton R, Ray G, Weddle D . Inversion of (R)- to (S)-ketoprofen in eight animal species. Chirality. 1995; 7(5):383-7. DOI: 10.1002/chir.530070513. View

18.

Miranda H, Puig M, Dursteler C, Prieto J, Pinardi G . Dexketoprofen-induced antinociception in animal models of acute pain: synergy with morphine and paracetamol. Neuropharmacology. 2006; 52(2):291-6. DOI: 10.1016/j.neuropharm.2006.07.025. View

19.

Jamali F, Lovlin R, Aberg G . Bi-directional chiral inversion of ketoprofen in CD-1 mice. Chirality. 1997; 9(1):29-31. DOI: 10.1002/(SICI)1520-636X(1997)9:1<29::AID-CHIR6>3.0.CO;2-B. View

20.

Agner T, Serup J . Sodium lauryl sulphate for irritant patch testing--a dose-response study using bioengineering methods for determination of skin irritation. J Invest Dermatol. 1990; 95(5):543-7. DOI: 10.1111/1523-1747.ep12504896. View