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image of Development of Nanoemulsion-Based Gel of Betulin for the Treatment of Psoriasis-Like Skin Inflammation in a Small Animal Model

Abstract

Introduction/ Background

This study aimed to introduce a gel (NEG) formulation containing betulin-loaded nanoemulsions for topical psoriasis treatment.

Materials and Methods

The prepared nanoemulsions were optimized for smaller particle size and higher drug content using a response surface methodology that exhibited uniform distribution and high drug loading (21.17±3.55%).

Results

The gel demonstrated skin-compatible pH and good spreadability. The developed gel showed slower release compared to nanoemulsion. pharmacokinetics demonstrated elevated AUC (55835.1 µg/cm2.h) and extended Tmax (720 min) for the gel than NE, indicating extended skin retention. Improved skin hydration (35%) and lipid content (28%) were observed, along with significant reductions in PASI scores and cytokine levels.

Discussion

Provided with enhanced skin retention, improved hydration, and lipid content, along with significant therapeutic efficacy in psoriasis treatment, betulin-loaded nanoemulsion gel demonstrated prolonged drug release and notably reduced PASI scores and cytokine levels, highlighting its effectiveness against psoriasis.

Conclusion

This highlights the promising potential of NEG for topical psoriasis management.

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2024-12-30
2025-11-05

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References

  1. Anonymous IFPA applauds WHO report on psoriasis and WHO EB adoption of resolution. IFPA Stockholm, Sweden 2013a
    [Google Scholar]
  2. Anonymous IFPA welcomes WHO member state efforts to raise awareness for psoriasis. IFPA Stockholm, Sweden 2013b
    [Google Scholar]
  3. Anonymous IFPA, IPC and ILDS form partnership to develop Global Psoriasis Atlas. DOI Stockholm, Sweden 2014
    [Google Scholar]
  4. Zhao Y. Sun J. Dou W. Hu J-H. Curcumin inhibits proliferation of interleukin-22-treated HaCaT cells. Int. J. Clin. Exp. Med. 2015 8 6 9580 9584 26309628
    [Google Scholar]
  5. Poligone B. Ghosh S. Method of preventing development of psoriatic lesions. Patent WO2012154684 2014
  6. Rai V.K. Sharma A. Upadhyay D.K. Gupta G.D. Narang R.K. IL-23/Th17 axis: A potential therapeutic target of psoriasis. Curr. Drug Res. Rev. 2022 14 1 24 36 10.2174/2589977513666210707114520 34238181
    [Google Scholar]
  7. Biswasroy P. Pradhan D. Sahu D.K. Rai V. Halder J. Rajwar T.K. Bhola R.K. Kar B. Ghosh G. Rath G. Phytochemical investigation, structural elucidation, in silico study and anti-psoriatic activity of potent bioactive from Betula utilis. J. Biomol. Struct. Dyn. 2023 41 17 8093 8108 10.1080/07391102.2022.2130981 36214696
    [Google Scholar]
  8. Dubinin M.V. Semenova A.A. Ilzorkina A.I. Markelova N.Y. Penkov N.V. Shakurova E.R. Belosludtsev K.N. Parfenova L.V. New quaternized pyridinium derivatives of betulin: Synthesis and evaluation of membranotropic properties on liposomes, pro- and eukaryotic cells, and isolated mitochondria. Chem. Biol. Interact. 2021 349 109678 10.1016/j.cbi.2021.109678 34600868
    [Google Scholar]
  9. Hussain A. Samad A. Singh S.K. Ahsan M.N. Haque M.W. Faruk A. Ahmed F.J. Nanoemulsion gel-based topical delivery of an antifungal drug: In vitro activity and in vivo evaluation. Drug Deliv. 2015 2015 1 16 10.3109/10717544.2014.933284 25013957
    [Google Scholar]
  10. Ahmad M.Z. Ahmad J. Alasmary M.Y. Akhter S. Aslam M. Pathak K. Jamil P. Abdullah M.M. Nanoemulgel as an approach to improve the biopharmaceutical performance of lipophilic drugs: Contemporary research and application. J. Drug Deliv. Sci. Technol. 2022 72 103420 10.1016/j.jddst.2022.103420
    [Google Scholar]
  11. Kuril A.K. Saravanan K. Method development and validation for the determination of higher molecular weight species of calcitonin salmon in calcitonin salmon injection by high performance size exclusion chromatography. Int. J. Pharm. Sci. Drug Res. 2024 260 266 10.25004/IJPSDR.2024.160216
    [Google Scholar]
  12. Sharma A. Upadhyay D.K. Sarma G.S. Kaur N. Gupta G.D. Narang R.K. Rai V.K. Squalene integrated NLC based gel of tamoxifen citrate for efficient treatment of psoriasis: A preclinical investigation. J. Drug Deliv. Sci. Technol. 2020 56 101568 10.1016/j.jddst.2020.101568
    [Google Scholar]
  13. Sandhu P.S. Beg S. Katare O.P. Singh B. QbD-driven development and validation of a HPLC method for estimation of tamoxifen citrate with improved performance. J. Chromatogr. Sci. 2016 54 8 1373 1384 10.1093/chromsci/bmw090 27226463
    [Google Scholar]
  14. Ravi P.R. Vats R. Dalal V. Gadekar N. N A. Design, optimization and evaluation of poly- ɛ -caprolactone (PCL) based polymeric nanoparticles for oral delivery of lopinavir. Drug Dev. Ind. Pharm. 2015 41 1 131 140 10.3109/03639045.2013.850710 24180260
    [Google Scholar]
  15. Chaudhary H. Kohli K. Amin S. Rathee P. Kumar V. Optimization and formulation design of gels of diclofenac and curcumin for transdermal drug delivery by box-behnken statistical design. J. Pharm. Sci. 2011 100 2 580 593 10.1002/jps.22292 20669331
    [Google Scholar]
  16. Rai V.K. Yadav N.P. Sinha P. Mishra N. Luqman S. Dwivedi H. Kymonil K.M. Saraf S.A. Development of cellulosic polymer based gel of novel ternary mixture of miconazole nitrate for buccal delivery. Carbohydr. Polym. 2014 103 126 133 10.1016/j.carbpol.2013.12.019 24528709
    [Google Scholar]
  17. Aljuffali I.A. Sung C.T. Shen F.M. Huang C.T. Fang J.Y. Squarticles as a lipid nanocarrier for delivering diphencyprone and minoxidil to hair follicles and human dermal papilla cells. AAPS J. 2014 16 1 140 150 10.1208/s12248‑013‑9550‑y 24307611
    [Google Scholar]
  18. Srivastava N. Patel D.K. Rai V.K. Pal A. Yadav N.P. Development of emulgel formulation for vaginal candidiasis: Pharmaceutical characterization, in vitro and in vivo evaluation. J. Drug Deliv. Sci. Technol. 2018 48 490 498 10.1016/j.jddst.2018.10.013
    [Google Scholar]
  19. Alam M. Mishra A. Yadav K.S. Pradhan D. Kar B. Ghosh G. Rath G. Rai V.K. Development and evaluation of dutasteride nanoemulgel for the topical delivery against Androgenic alopecia. Pharm. Nanotechnol. 2024 12 5 459 470 10.2174/0122117385269151231031161411 38173065
    [Google Scholar]
  20. Sharma A. Mehta V. Parashar A. Patrwal R. Malairaman U. Solid lipid nanoparticle: Fabricated through nanoprecipitation and their physicochemical characterization. Int. J. Pharm. Pharm. Sci. 2016 8 10 144 148 10.22159/ijpps.2016v8i10.13207
    [Google Scholar]
  21. Joshi N. Mishra N. Rai V.K. Development and evaluation of in situ gel of silver sulfadiazine for improved therapeutic efficacy against infectious burn wound. J. Pharm. Innov. 2021 16 3 537 550 10.1007/s12247‑020‑09464‑y
    [Google Scholar]
  22. Kang R.K. Mishr N. Rai V.K. Guar gum micro-particles for targeted co-delivery of doxorubicin and metformin HCL for improved specificity and efficacy against colon cancer: In vitro and in vivo studies. AAPS Pharm. Sci. Tech. 2020 21 2 48 10.1208/s12249‑019‑1589‑3 31900731
    [Google Scholar]
  23. Sinha P. Srivastava N. Rai V.K. Mishra R. Ajayakumar P.V. Yadav N.P. A novel approach for dermal controlled release of salicylic acid for improved anti-inflammatory action: Combination of hydrophilic-lipophilic balance and response surface methodology. J. Drug Deliv. Sci. Technol. 2019 52 870 884 10.1016/j.jddst.2019.06.007
    [Google Scholar]
  24. Mishra N. Yadav K.S. Rai V.K. Yadav N.P. Polysaccharide encrusted multilayered nano-colloidal system of andrographolide for improved hepatoprotection. AAPS Pharm. Sci. Tech. 2017 18 2 381 392 10.1208/s12249‑016‑0512‑4 27007741
    [Google Scholar]
  25. Mishra N. Rai V.K. Yadav K.S. Sinha P. Kanaujia A. Chanda D. Jakhmola A. Saikia D. Yadav N.P. Encapsulation of mentha oil in chitosan polymer matrix alleviates skin irritation. AAPS Pharm. Sci. Tech. 2016 17 2 482 492 10.1208/s12249‑015‑0378‑x 26248538
    [Google Scholar]
  26. Pandey A.K. Choudhary N. Rai V.K. Dwivedi H. Kymonil K.M. Saraf S.A. Fabrication and evaluation of tinidazole microbeads for colon targeting. Asian Pac. J. Trop. Dis. 2012 2 S197 S201 10.1016/S2222‑1808(12)60151‑0
    [Google Scholar]
  27. Nanda A. Nanda S. Nguyen T.A. Rajendran S. Slimani Y. Nanocosmetics: Fundamentals. Applications and Toxicity Elsevier 2020 483 503 10.1016/C2019‑0‑00468‑2
    [Google Scholar]
  28. Yadav N.P. Rai V.K. Mishra N. Sinha P. Bawankule D.U. Pal A. Tripathi A.K. Chanotiya C.S. A novel approach for development and characterization of effective mosquito repellent cream formulation containing citronella oil. BioMed Res. Int. 2014 2014 1 11 10.1155/2014/786084 25379509
    [Google Scholar]
  29. Upadhyay D.K. Sharma A. Kaur N. Gupta G.D. Narang R.K. Rai V.K. Nanoemulgel for efficient topical delivery of finasteride against Androgenic alopecia. J. Pharm. Innov. 2021 16 4 735 746 10.1007/s12247‑020‑09483‑9
    [Google Scholar]
  30. Saha I. Palak A. Rai V.K. Relevance of NLC-gel and microneedling-assisted tacrolimus ointment against severe psoriasiform: In vitro dermal retention kinetics, in vivo activity and drug distribution. J. Drug Deliv. Sci. Technol. 2022 71 103272 10.1016/j.jddst.2022.103272
    [Google Scholar]
  31. Incecayir T. Agabeyoglu I. Derici U. Sindel S. Assessment of topical bioequivalence using dermal microdialysis and tape stripping methods. Pharm. Res. 2011 28 9 2165 2175 10.1007/s11095‑011‑0444‑3 21499834
    [Google Scholar]
  32. Rai V.K. Kumar A. Pradhan D. Halder J. Rajwar T.K. Sarangi M.K. Dash P. Das C. Manoharadas S. Kar B. Ghosh G. Rath G. Spray-dried mucoadhesive re-dispersible gargle of chlorhexidine for improved response against throat infection: formulation development, in vitro and in vivo evaluation. AAPS Pharm. Sci. Tech. 2024 25 2 31 10.1208/s12249‑024‑02750‑9 38326518
    [Google Scholar]
  33. Akhtar N. Khan A.B. Muhammad S. Ahmed M. Khan H.M.S. Rasool F. Saeed T. Formulation and characterization of a cream containing terminalia chebula extract. Forsch. Komplement. Med. 2012 19 1 20 25 10.1159/000335823 22398922
    [Google Scholar]
  34. van der Fits L. Mourits S. Voerman J.S.A. Kant M. Boon L. Laman J.D. Cornelissen F. Mus A.M. Florencia E. Prens E.P. Lubberts E. Imiquimod-induced psoriasis-like skin inflammation in mice is mediated via the IL-23/IL-17 axis. J. Immunol. 2009 182 9 5836 5845 10.4049/jimmunol.0802999 19380832
    [Google Scholar]
  35. Sun J. Zhao Y. Hu J. Curcumin inhibits imiquimod-induced psoriasis-like inflammation by inhibiting IL-1beta and IL-6 production in mice. PLoS One 2013 8 6 e67078 10.1371/journal.pone.0067078 23825622
    [Google Scholar]
  36. Na Takuathung M Wongnoppavich A Panthong A Khonsung P Chiranthanut N. Antipsoriatic effects of wannachawee recipe on imiquimod-induced psoriasis-like dermatitis in BALB/c mice. Evid. Based Complement. Alternat. Med. 2018 2018 7931031 10.1155/2018/7931031 29619073
    [Google Scholar]
  37. Schneider M. Stracke F. Hansen S. Schaefer U.F. Nanoparticles and their interactions with the dermal barrier. Dermatoendocrinol 2009 1 4 197 206 10.4161/derm.1.4.9501 20592791
    [Google Scholar]
  38. Weber S. Zimmer A. Pardeike J. Solid lipid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) for pulmonary application: A review of the state of the art. Eur. J. Pharm. Biopharm. 2014 86 1 7 22 10.1016/j.ejpb.2013.08.013 24007657
    [Google Scholar]
  39. Alexander A. Dwivedi S. Ajazuddin Giri T.K. Saraf S. Saraf S. Tripathi D.K. Approaches for breaking the barriers of drug permeation through transdermal drug delivery. J. Control. Release 2012 164 1 26 40 10.1016/j.jconrel.2012.09.017 23064010
    [Google Scholar]
  40. Rai V.K. Roy A. Sharma A. Rath G. Kar B. Ghosh G. Pradhan D. Halder J. Development and pharmaceutical evaluation of azelaic acid and vitamin E oil-based nanoemulgel of tacrolimus for topical application in plaque psoriasis. J. Pharm. Innov. 2023 18 4 1616 1625 10.1007/s12247‑023‑09740‑7
    [Google Scholar]
  41. Kraft J.N. Lynde C.W. Moisturizers: what they are and a practical approach to product selection. Skin Therapy Lett. 2005 10 5 1 8 15986082
    [Google Scholar]
  42. Papakostas D. Rancan F. Sterry W. Blume-Peytavi U. Vogt A. Nanoparticles in dermatology. Arch. Dermatol. Res. 2011 303 8 533 550 10.1007/s00403‑011‑1163‑7 21837474
    [Google Scholar]
  43. Knaggs H.E. Wood E.J. Rizer R.L. Mills O.H. Post‐adolescent acne. Int. J. Cosmet. Sci. 2004 26 3 129 138 10.1111/j.1467‑2494.2004.00210.x 18494869
    [Google Scholar]
  44. Rai V.K. Chanda D. Chanotiya C.S. Yadav N.P. A combination of linalool and linalyl acetate synergistically alleviates imiquimod-induced psoriasis-like skin inflammation in BALB/c mice. Front. Pharmacol. 2022 13 913174 10.3389/fphar.2022.913174 35991888
    [Google Scholar]
  45. Rai V.K. Sinha P. Yadav K.S. Shukla A. Saxena A. Bawankule D.U. Tandon S. Khan F. Chanotiya C.S. Yadav N.P. Anti-psoriatic effect of Lavandula angustifolia essential oil and its major components linalool and linalyl acetate. J. Ethnopharmacol. 2020 261 113127 10.1016/j.jep.2020.113127 32623016
    [Google Scholar]
  46. Behjati S. Frank M. The effects of tamoxifen on immunity. Curr. Med. Chem. 2009 16 24 3076 3080 10.2174/092986709788803042 19689284
    [Google Scholar]
/content/journals/pnt/10.2174/0122117385336297241210053845
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Development of Nanoemulsion-Based Gel of Betulin for the Treatment of Psoriasis-Like Skin Inflammation in a Small Animal Model
Bentham Science Publishers ; https://doi.org/10.2174/0122117385336297241210053845
/content/journals/pnt/10.2174/0122117385336297241210053845
/content/journals/pnt/10.2174/0122117385336297241210053845
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  • Article Type:     Research Article
Keywords: betulin ; nanoemulsion ; topical ; emulgel ; Psoriasis ; gel

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