{"title":"非那雄胺负载型聚乳酸(PLGA)纳米颗粒(载Carbopol凝胶)用于刺激毛发生长治疗的优化和经叶脉给药","authors":"Mounika Kuchukuntla, Venkatesan Palanivel, Ananthula Madhubabu","doi":"10.2174/0115734072269998240101043601","DOIUrl":null,"url":null,"abstract":"\n\nOne of the frequent side effects of cancer treatment is chemotherapyinduced alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor, has\nshown tremendous promise in therapeutic uses for treating baldness. Still, systemic side effects constrained its broad use in alopecia from oral treatment and a low absorption rate at the target site—\nPLGA-loaded nanoparticles (NPs) for topical delivery of FNS—to overcome these issues.\n\n\n\nThe nano-precipitation process was used to make FNS-NPs. The independent variables\n(stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on the\npoint prediction method obtainable by the Box Behnken design software, the best FNS-NPs composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal FNS-NPs\ncomposition was further transformed into a gel formulation. The prepared topical gel formulation\n(FNS-NPs gel) included gel characterization, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry\n(DSC), Fourier Transform Infrared Spectroscopy (FTIR), invitro and in vivo studies.\n\n\n\nOptimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI,\n71.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and\nthe excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content,\nviscosity, pH, and spreadability. According to the release and permeation investigation findings,\nFNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before.\nIn a dose- and time-dependent manner, the produced nanoparticles considerably (p≤0.05) increased FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel\nshowed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery mechanism of the FNS-NPs gel might stimulate hair growth.\n\n\n\nThese findings imply that the innovative formulation that has been developed has several\nbeneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata\n","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"14 4","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Optimization and Transfollicular Delivery of Finasteride Loaded PLGA Nanoparticles Laden Carbopol Gel for Treatment of Hair Growth Stimulation\",\"authors\":\"Mounika Kuchukuntla, Venkatesan Palanivel, Ananthula Madhubabu\",\"doi\":\"10.2174/0115734072269998240101043601\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"\\n\\nOne of the frequent side effects of cancer treatment is chemotherapyinduced alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor, has\\nshown tremendous promise in therapeutic uses for treating baldness. Still, systemic side effects constrained its broad use in alopecia from oral treatment and a low absorption rate at the target site—\\nPLGA-loaded nanoparticles (NPs) for topical delivery of FNS—to overcome these issues.\\n\\n\\n\\nThe nano-precipitation process was used to make FNS-NPs. The independent variables\\n(stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on the\\npoint prediction method obtainable by the Box Behnken design software, the best FNS-NPs composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal FNS-NPs\\ncomposition was further transformed into a gel formulation. The prepared topical gel formulation\\n(FNS-NPs gel) included gel characterization, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry\\n(DSC), Fourier Transform Infrared Spectroscopy (FTIR), invitro and in vivo studies.\\n\\n\\n\\nOptimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI,\\n71.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and\\nthe excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content,\\nviscosity, pH, and spreadability. According to the release and permeation investigation findings,\\nFNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before.\\nIn a dose- and time-dependent manner, the produced nanoparticles considerably (p≤0.05) increased FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel\\nshowed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery mechanism of the FNS-NPs gel might stimulate hair growth.\\n\\n\\n\\nThese findings imply that the innovative formulation that has been developed has several\\nbeneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata\\n\",\"PeriodicalId\":10772,\"journal\":{\"name\":\"Current Bioactive Compounds\",\"volume\":\"14 4\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-01-19\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Bioactive Compounds\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/0115734072269998240101043601\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Bioactive Compounds","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/0115734072269998240101043601","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
Optimization and Transfollicular Delivery of Finasteride Loaded PLGA Nanoparticles Laden Carbopol Gel for Treatment of Hair Growth Stimulation
One of the frequent side effects of cancer treatment is chemotherapyinduced alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor, has
shown tremendous promise in therapeutic uses for treating baldness. Still, systemic side effects constrained its broad use in alopecia from oral treatment and a low absorption rate at the target site—
PLGA-loaded nanoparticles (NPs) for topical delivery of FNS—to overcome these issues.
The nano-precipitation process was used to make FNS-NPs. The independent variables
(stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on the
point prediction method obtainable by the Box Behnken design software, the best FNS-NPs composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal FNS-NPs
composition was further transformed into a gel formulation. The prepared topical gel formulation
(FNS-NPs gel) included gel characterization, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry
(DSC), Fourier Transform Infrared Spectroscopy (FTIR), invitro and in vivo studies.
Optimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI,
71.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and
the excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content,
viscosity, pH, and spreadability. According to the release and permeation investigation findings,
FNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before.
In a dose- and time-dependent manner, the produced nanoparticles considerably (p≤0.05) increased FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel
showed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery mechanism of the FNS-NPs gel might stimulate hair growth.
These findings imply that the innovative formulation that has been developed has several
beneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata
Current Bioactive CompoundsPharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.90
自引率
0.00%
发文量
112
期刊介绍:
The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.