Proniosomal transdermal therapeutic system of losartan potassium: Development and pharmacokinetic evaluation

ArticleinJournal of Drug Targeting 17(6):442-9 · August 2009with37 Reads
DOI: 10.1080/10611860902963039 · Source: PubMed
Abstract
The purpose of the current study was to investigate the feasibility of proniosomes as transdermal drug delivery system for losartan potassium. Different preparations of proniosomes were fabricated using different nonionic surfactants, such as Span 20, Span 40, Span 60, Span 80, Tween 20, Tween 40, and Tween 80. Different formulae were prepared and coded as PNG-1 (proniosomal gel-1) to PNG-7. The best in vitro skin permeation profile was obtained with proniosomal formulation PNG-2 in 24 h. The permeability parameters such as flux, permeability coefficient, and enhancement ratio were significant for PNG-2 compared with other formulations (P < 0.05). This optimized PNG-2 was fabricated in the form of transdermal patch using HPMC gel as a suitable base. Proniosomal transdermal therapeutic system (PNP-H) was found to be the optimized one as it gave better release of drug and better permeation in a steady-state manner over a desired period of time, that is, 24 h through rat skin. In vivo pharmacokinetic study of PNP-H showed a significant increase in bioavailability (1.93 times) compared with oral formulation of losartan potassium. The formulation appeared to be stable when stored at room temperature (30 +/- 2 degrees C) and at refrigeration temperature (4 +/- 2 degrees C) for 45 days.
    • "Petkar and Kuchekar examined the influence of capsaicin in transdermal transport of losartan (Petkar and Kuchekar, 2007). The use of proniosomes to facilitate transdermal transport of losartan has also been reported by Thakur and coworker (Thakur et al., 2009). Furthermore, none of those studies were concerned on the transport mechanism of transdermal delivery of losartan. "
    Article · Apr 2014
    • "In recent time, proniosome has been received a great attention for delivering the drug substances via transdermal route as transdermal administration of drug avoids some drawbacks unlike oral route. Both hydrophilic and lipophilic drugs like: losartan potassium [47], chlorpheniramine maleate [48], levonorgestrel [35], flurbiprofen [49], ketoprofen [50], captopril [33], celecoxib [51], piroxicam [1, 52], carvediol [53], methotrexate [54], doxorubicin [55] have been found high permeation efficiency through the skin. Proniosomal preparation now has been used in cosmetics. "
    Full-text · Article · Nov 2011 · International Journal of Drug Development & Research
    • "This will increase the increases the concentration gradient and hence increases the diffusion pressure for the driving of drug through the stratum corneum. Estradiol [18] Chlorpheniramine Maleate [19] Ketoprofen [37] Contraceptive agent Piroxicam [38] Celecoxib [42] Tenoxicam [27] Captopril [43] Frusemide [35] Losartan potassium [39] Hydrocorticosone [4 4] Vinpocetine [15] NSAIDs The study showed that 1% proniosomal gel showed greater anti-inflammatory activity than the marketed 1% hydrocortisone gel. Hence, prolong the action. "
    [Show abstract] [Hide abstract] ABSTRACT: Skin has become an impressive and idealistic platform for the delivery of drugs compared to other routes. However, the stratum corneum "dead, impermeable barrier devoid of biological activity" to skin had challenged the development of transdermal product, which delivers the drugs directly to the systemic circulation at a controlled rate [1]. Several approaches put forward to enhance the penetration of drug through skin for transdermal drug delivery and one among them are provesicular niosomes (proniosomes), which ideally possess the sole property of reversibly reducing the barrier resistance of the horny layer, allowing the drug to reach the living tissues at a greater rate. The provesicular niosomes (non-ionic surfactant based vesicles); colloid carrier is still in its infancy and need to exploit more in field of drug delivery. These vesicles are formed from the self-assembly of non-ionic amphiphiles in aqueous medium results in closed bilayer structure which can entraps both lipophilic and hydrophilic drugs [2]. They are non-toxic and non-immunogenic bilayer that be converted to niosomes when applied to skin by in-situ absorption of water and interacts with the strong hydrogen bond of stratum corneum and loosens it, thereby allowing the diffusion of drug into the skin. It also possesses enhanced stability compared to other vesicular carrier. This review is an insight into the exploitation of the various properties of drug to encapsulated, preparation, mechanism of penetration and application in transdermal drug delivery. The factor affecting the entrapment and penetration of drug through the skin also reviewed.
    Article · Jul 2011
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