<i>In Vitro</i> Permeation of Micronized and Nanonized Alaptide from Semisolid Formulations

Opatřilová, Radka; Černíková, Aneta; Coufalová, Lenka; Dohnal, Jiří; Jampílek, Josef

doi:10.1155/2013/787283

Cited by 16 publications

(8 citation statements)

References 42 publications

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“…Furthermore, the permeation of micronized (ALA) and nanonized (NALA) alaptide alone through the full-thickness pig ear skin from various semi-solid compositions was evaluated and different behaviour among both forms was confirmed. Though permeation of NALA through the skin was limited compared with ALA [34], NALA was also positively evaluated as a potential modifier of transdermal permeation [32,33]. Thus, the aim of this primary rapid study was to evaluate the effect of alaptide in micronized and nanonized forms on drug permeation through the skin immediately after application of the drug formulation.…”

Section: Introductionmentioning

confidence: 99%

Rapid Screening of Mupirocin Skin Permeation Modification by Micronized and Nanonized Alaptide

Jampílek

Opatřilová

2014

ADMET DMPK

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The investigation deals with the affection of permeation of mupirocin from the Bactroban® Leciva ointment through full-thickness pig ear skin by alaptide that was applied in micronized or nanonized form as a potential excipient. Alaptide, (S)-8-methyl-6,9-diazaspiro[4.5]decan-7,10-dione, was the original Czech compound. It was discovered that micronized alaptide significantly enhanced the permeation of mupirocin within 1 h after administration (approx. 5-fold). On the other hand, nanonized alaptide almost completely inhibited permeation of mupirocin from Bactroban® Leciva through the skin.Rapid primary screening showed that the two forms of alaptide differently influenced the depth and the rate of permeation/penetration of mupirocin into/through the skin, i.e., affect curative effect of mupirocin on/in skin immediately after application of drug formulation.

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Section: Introductionmentioning

confidence: 99%

Rapid Screening of Mupirocin Skin Permeation Modification by Micronized and Nanonized Alaptide

Jampílek

Opatřilová

2014

ADMET DMPK

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“…Alaptide is a spirocyclic dipeptide, which was designed as an analogue of melanocyte-stimulating hormone release-inhibiting factor (MIF) and synthesized by Kasafirek et al at the Research Institute for Pharmacy and Biochemistry in Prague, Czechoslovakia, in the 1980s of the twentieth century [68]. Alaptide showed a great potential for regeneration of the injured skin and also for enhanced transdermal penetration of drugs [69,70]. Arginine is amino acid which is a precursor of nitric oxide, implicated in wound healing.…”

Section: Nanofibers From Synthetic Degradable Polymersmentioning

confidence: 99%

Nanofibrous Scaffolds for Skin Tissue Engineering and Wound Healing Based on Synthetic Polymers

Bačáková¹,

Zikmundová²,

Pajorová³

et al. 2020

Applications of Nanobiotechnology

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Nanofibrous scaffolds are popular materials in all areas of tissue engineering, because they mimic the fibrous component of the natural extracellular matrix. In this chapter, we focused on the application of nanofibers in skin tissue engineering and wound healing, because the skin is an organ with several vitally important functions, particularly barrier, thermoregulatory, and sensory functions. Nanofibrous meshes not only serve as carriers for skin cells but also can prevent the penetration of microbes into wounds and can keep appropriate moisture in the damaged skin. The nanofibrous meshes have been prepared from a wide range of synthetic and nature-derived polymers. This review is concentrated on synthetic non-degradable and degradable polymers, which have been explored for skin tissue engineering and wound healing. These synthetic polymers were often combined with natural polymers of the protein or polysaccharide nature, which improved their attractiveness for cell colonization. The nanofibrous scaffolds can also be loaded with various bioactive molecules, such as growth factors, hormones, vitamins, antioxidants, antimicrobial, and antitumor agents. In advanced tissue engineering approaches, the cells on the nanofibrous scaffolds are cultured in dynamic bioreactors enabling appropriate mechanical stimulation of cells and at air-liquid interface. This chapter summarizes recent results achieved in the field of nanofiber-based skin tissue engineering, including results of our research group.

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“…The rotor speed was increased to 1500 rpm after 6 h of milling. The total time of milling was 57.5 h. The content of alaptide in the suspension was 38.76 g/L (determined by RP-HPLC [11]). The particle size of the prepared nanonized alaptide was measured by Sympatec NANOPHOX 0138 P (Germany), and the particle size x 90 was 770 nm.…”

Section: Preparation Of Nanonized Alaptidementioning

confidence: 99%

Rapid Informative Screening of Nano-Alaptide as Potential Transdermal Permeation Enhancer of Acetylsalicylic Acid and Paracetamol

Černíková¹,

Opatřilová²,

Jampílek³

2014

Mil. Med. Sci. Lett.

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This investigation deals with the affection of permeation of acetylsalicylic acid and paracetamol applied in the system propylene glycol-water 1:1 through full-thickness pig ear skin by alaptide that was applied in nanonized form as a potential chemical penetration enhancer. Alaptide, (S)-8-methyl-6,9diazaspiro[4.5]decan-7,10-dione, is the original Czech compound. The application of nanonized alaptide significantly enhanced the permeation of both drugs through the skin. Enhancement ratios in the studied time interval 0.5-2.0 h varied from 1.11 to 17.70 for acetylsalicylic acid and from 6.83 to 19.83 for paracetamol.

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In Vitro Permeation of Micronized and Nanonized Alaptide from Semisolid Formulations

Cited by 16 publications

References 42 publications

Rapid Screening of Mupirocin Skin Permeation Modification by Micronized and Nanonized Alaptide

Rapid Screening of Mupirocin Skin Permeation Modification by Micronized and Nanonized Alaptide

Nanofibrous Scaffolds for Skin Tissue Engineering and Wound Healing Based on Synthetic Polymers

Rapid Informative Screening of Nano-Alaptide as Potential Transdermal Permeation Enhancer of Acetylsalicylic Acid and Paracetamol

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