Amit Pratap Singh, Sushil Kumar Kashaw, Vandana Soni
{"title":"他沙罗汀治疗痤疮乳状剂的设计、优化及体内评价。","authors":"Amit Pratap Singh, Sushil Kumar Kashaw, Vandana Soni","doi":"10.1080/1061186X.2025.2546489","DOIUrl":null,"url":null,"abstract":"<p><p>Acne vulgaris is a common dermatological disorder, with current treatments often limited to poor skin penetration, instability, irritation and suboptimal therapeutic outcomes. There is a pressing need for advanced drug delivery systems that can overcome these limitations and enhance treatment efficacy. This study aimed to develop and optimise a novel tazarotene-loaded emulgel formulation, combining the advantages of emulsions and gels to achieve controlled drug release, improved stability and superior clinical performance in topical acne therapy. The formulation was prepared using the incorporation method and optimised through the Box-Behnken statistical design (BBD). Three independent variables, such as Carbopol 940 (<i>X</i><sub>1</sub>), Span 80 (<i>X</i><sub>2</sub>) and Tween 80 (<i>X</i><sub>3</sub>), were assessed for their effects on drug release (<i>Y</i><sub>1</sub>) and viscosity (<i>Y</i><sub>2</sub>). The optimised formulation exhibited desirable characteristics, including pH: 6.6 ± 0.3, viscosity: 28,945 cPs, spreadability: 6.17 ± 0.02 cm<sup>2</sup>, extrudability: 18 ± 2.49 g/cm<sup>2</sup> and drug content: 85.46 ± 4.02%. <i>In vitro</i> studies demonstrated 87.59 ± 2.6% drug release over 7 h. A skin irritation test in mice confirmed its dermatological safety, with no signs of erythema or oedema. Anti-acne efficacy, evaluated using a <i>Propionibacterium acnes</i>-induced murine model, revealed complete lesion clearance, outperforming a marketed gel. These findings firmly establish the tazarotene-loaded emulgel as a safe, effective, and superior topical treatment for acne.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-9"},"PeriodicalIF":3.9000,"publicationDate":"2025-08-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, optimisation and <i>in vivo</i> evaluation of tazarotene loaded emulgel formulation for the treatment of acne.\",\"authors\":\"Amit Pratap Singh, Sushil Kumar Kashaw, Vandana Soni\",\"doi\":\"10.1080/1061186X.2025.2546489\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Acne vulgaris is a common dermatological disorder, with current treatments often limited to poor skin penetration, instability, irritation and suboptimal therapeutic outcomes. There is a pressing need for advanced drug delivery systems that can overcome these limitations and enhance treatment efficacy. This study aimed to develop and optimise a novel tazarotene-loaded emulgel formulation, combining the advantages of emulsions and gels to achieve controlled drug release, improved stability and superior clinical performance in topical acne therapy. The formulation was prepared using the incorporation method and optimised through the Box-Behnken statistical design (BBD). Three independent variables, such as Carbopol 940 (<i>X</i><sub>1</sub>), Span 80 (<i>X</i><sub>2</sub>) and Tween 80 (<i>X</i><sub>3</sub>), were assessed for their effects on drug release (<i>Y</i><sub>1</sub>) and viscosity (<i>Y</i><sub>2</sub>). The optimised formulation exhibited desirable characteristics, including pH: 6.6 ± 0.3, viscosity: 28,945 cPs, spreadability: 6.17 ± 0.02 cm<sup>2</sup>, extrudability: 18 ± 2.49 g/cm<sup>2</sup> and drug content: 85.46 ± 4.02%. <i>In vitro</i> studies demonstrated 87.59 ± 2.6% drug release over 7 h. A skin irritation test in mice confirmed its dermatological safety, with no signs of erythema or oedema. Anti-acne efficacy, evaluated using a <i>Propionibacterium acnes</i>-induced murine model, revealed complete lesion clearance, outperforming a marketed gel. These findings firmly establish the tazarotene-loaded emulgel as a safe, effective, and superior topical treatment for acne.</p>\",\"PeriodicalId\":15573,\"journal\":{\"name\":\"Journal of Drug Targeting\",\"volume\":\" \",\"pages\":\"1-9\"},\"PeriodicalIF\":3.9000,\"publicationDate\":\"2025-08-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Drug Targeting\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/1061186X.2025.2546489\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Drug Targeting","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/1061186X.2025.2546489","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Design, optimisation and in vivo evaluation of tazarotene loaded emulgel formulation for the treatment of acne.
Acne vulgaris is a common dermatological disorder, with current treatments often limited to poor skin penetration, instability, irritation and suboptimal therapeutic outcomes. There is a pressing need for advanced drug delivery systems that can overcome these limitations and enhance treatment efficacy. This study aimed to develop and optimise a novel tazarotene-loaded emulgel formulation, combining the advantages of emulsions and gels to achieve controlled drug release, improved stability and superior clinical performance in topical acne therapy. The formulation was prepared using the incorporation method and optimised through the Box-Behnken statistical design (BBD). Three independent variables, such as Carbopol 940 (X1), Span 80 (X2) and Tween 80 (X3), were assessed for their effects on drug release (Y1) and viscosity (Y2). The optimised formulation exhibited desirable characteristics, including pH: 6.6 ± 0.3, viscosity: 28,945 cPs, spreadability: 6.17 ± 0.02 cm2, extrudability: 18 ± 2.49 g/cm2 and drug content: 85.46 ± 4.02%. In vitro studies demonstrated 87.59 ± 2.6% drug release over 7 h. A skin irritation test in mice confirmed its dermatological safety, with no signs of erythema or oedema. Anti-acne efficacy, evaluated using a Propionibacterium acnes-induced murine model, revealed complete lesion clearance, outperforming a marketed gel. These findings firmly establish the tazarotene-loaded emulgel as a safe, effective, and superior topical treatment for acne.
期刊介绍:
Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs.
Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.