Research Article
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Year 2025, Volume: 29 Issue: 3, 1209 - 1226, 04.06.2025
https://doi.org/10.12991/jrespharm.1694393

Abstract

References

  • [1]Kainz K, Bauer MA, Madeo F, Carmona-Gutierrez D. Fungal infections in humans: The silent crisis. Microbial Cell. 2020;7(6):143–145. https://doi.org/10.15698%2Fmic2020.06.718
  • [2]Charles AJ. Superficial cutaneous fungal infections in tropical countries. Dermatol Ther. 2009;22(6):550–559. https://doi.org/10.1111/j.1529-8019.2009.01276.x
  • [3]Ameen M. Epidemiology of superficial fungal infections. Clin Dermatol. 2010;28(2):197–201. https://doi.org/10.1016/j.clindermatol.2009.12.005
  • [4]Hay R. Superficial fungal infections. Medicine. 2013;41(12):716-718. https://doi.org/10.1016/j.mpmed.2013.09.011
  • [5]Karri VN, Raman SK, Kuppusamy G, Mulukutla S, Ramaswamy S, Malayandi R. Terbinafine hydrochloride loaded nanoemulsion based gel for topical application. J Pharm Investig. 2015;45:79-89. http://dx.doi.org/10.1007/s40005-014-0149-9
  • [6]Loftsson T. Drug stability for pharmaceutical scientists. Academic press; 2014 Jan 25.
  • [7]Shrestha S, Pokhrel S, Sharma S, Manandhar M, Alam I. Formulation and evaluation of topical microemulgel loaded with terbinafine HCl microemulsion. Int J Pharm Sci Res. 2017;26:4716-4723. http://dx.doi.org/10.13040/IJPSR.0975-8232.8 (11).4716-23
  • [8]Alberti I, Kalia YN, Naik A, Bonny JD, Guy RH. In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum. J Control Release. 2001;71(3):319–327. https://doi.org/10.1016/s0168-3659(01)00244-9
  • [9]Balfour JA, Faulds D. Terbinafine: A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial mycoses. Drugs. 1992;43:259-284.https://doi.org/10.2165/00003495-199243020-00010
  • [10]Kazakov PV, Golosov SN. A Simple method for obtaining terbinafine hydrochloride. Pharm Chem J. 2004 ;38(4):206–208. https://doi.org/10.1023/B%3APHAC.0000038420.81588.50
  • [11]Hossain AM, Sil BC, Iliopoulos F, Lever R, Hadgraft J, Lane ME. Preparation, characterisation, and topical delivery of terbinafine. Pharmaceutics. 2019;11(10):548. https://doi.org/10.3390/pharmaceutics11100548
  • [12]Thavva VE, Baratam SR. Formulation and evaluation of terbinafine hydrochloride microsponge gel. Int J Appl Pharm. 2019;11(6):78-85. http://dx.doi.org/10.22159/ijap.2019v11i6.32502
  • [13]Nangare S, Dugam S. Smart invasome synthesis, characterizations, pharmaceutical applications, and pharmacokinetic perspective: a review. Future J Pharm Sci. 2020;6(1):1-21. https://doi.org/10.1186/s43094-020-00145-8
  • [14]Dragicevic-Curic N, Gräfe S, Albrecht V, Fahr A. Topical application of temoporfin-loaded invasomes for photodynamic therapy of subcutaneously implanted tumours in mice: a pilot study. J Photochem Photobiol B: Biology. 2008;91(1):41-50. https://doi.org/10.1016/j.jphotobiol.2008.01.009
  • [15]Zellmer S, Pfeil W, Lasch J. Interaction of phosphatidylcholine liposomes with the human stratum corneum. Biochim Biophys Acta (BBA)-Biomembranes. 1995;1237(2):176-182. https://doi.org/10.1016/0005-2736(95)00100-h
  • [16]Cornwell PA, Barry BW, Bouwstra JA, Gooris GS. Modes of action of terpene penetration enhancers in human skin; differential scanning calorimetry, small-angle X-ray diffraction and enhancer uptake studies. Int J Pharm. 1996;127(1):9-26. https://doi.org/10.1016/0378-5173(95)04108-7
  • [17]Kamran M, Ahad A, Aqil M, Imam SS, Sultana Y, Ali A. Design, formulation and optimization of novel soft nano-carriers for transdermal olmesartan medoxomil delivery: In vitro characterization and in vivo pharmacokinetic assessment. Int J Pharm. 2016;505(1-2):147-158. https://doi.org/10.1016/j.ijpharm.2016.03.030
  • [18]Prasanthi D, K Lakshmi P. Iontophoretic transdermal delivery of finasteride in vesicular invasomal carriers. Pharm Nanotechnol. 2013;1(2):136-150. http://dx.doi.org/10.2174/2211738511301020009
  • [19]Babaie S, Del Bakhshayesh AR, Ha JW, Hamishehkar H, Kim KH. Invasome: A novel nanocarrier for transdermal drug delivery. Nanomaterials. 2020;10(2):341. https://doi.org/10.3390/nano10020341
  • [20]Leite MC, Bezerra AP, Sousa JP, Guerra FQ, Lima ED. Evaluation of antifungal activity and mechanism of action of citral against Candida albicans. Evid-Based Complement Altern Med. 2014: 378280. https://doi.org/10.1155%2F2014%2F378280
  • [21]Han Y, Sun Z, Chen W. Antimicrobial susceptibility and antibacterial mechanism of limonene against Listeria monocytogenes. Molecules. 2019;25(1):33. https://doi.org/10.3390%2Fmolecules25010033
  • [22]Lakshmi PK, Mounica V, Manoj KY, Prasanthi D. Preparation and evaluation of curcumin invasomes. Int J Drug Deliv. 2014;6(2):113. http://www.arjournals.org/index.php/ijdd/index
  • [23]Chaudhari PD, Desai US. Formulation and evaluation of niosomal in situ gel of prednisolone sodium phosphate for ocular drug delivery. Int J Appl Pharm. 2019;97-116. https://doi.org/10.22159/ijap.2019v11i2.30667
  • [24]Mohite R, Mehta P, Arulmozhi S, Kamble R, Pawar A, Bothiraja C. Synthesis of fisetin co-crystals with caffeine and nicotinamide using the cooling crystallization technique: Biopharmaceutical studies. New J Chem. 2019;43(34):13471-13479. https://doi.org/10.1039/C9NJ01848D
  • [25]Kolhe SS. Evaluation of polyherbal ointment for wound healing activity in Wistar rats. J Drug Deliv Ther. 2018;8(6-s):26-31. https://doi.org/10.22270/jddt.v8i6-s.2072
  • [26]Maru AD, Lahoti SR. Formulation and evaluation of ointment containing sunflower wax. Asian J Pharm Clin Res. 2019;12(8):115-120. http://dx.doi.org/10.22159/ajpcr.2019.v12i18.33199
  • [27]Prasad SR, Elango K, Damayanthi D, Saranya JS. Formulation and evaluation of azathioprine loaded silver nanopartilces for the treatment of rheumatoid arthritis. Asian J Biomed Pharm Sci. 2013;3(23):28-32. https://doi.org/10.15272/AJBPS.V3I23.312
  • [28]Alase PP. Sustained ophthalmic delivery of gatifloxacin from in situ gelling system (Doctoral dissertation, Rajiv Gandhi University of Health Sciences (India)). 2006;814–8. http://dx.doi.org/10.4103/0250-474X.31025
  • [29]Satturwar PM, Fulzele SV, Nande VS, Khandare JN. Formulation and evaluation of ketoconazole niosomes. Indian J Pharm Sci. 2002;64(2):155-158.
  • [30]Amnuaikit T, Limsuwan T, Khongkow P, Boonme P. Vesicular carriers containing phenylethyl resorcinol for topical delivery system; liposomes, transfersomes and invasomes. Asian J Pharm Sci. 2018;13(5):472-484. https://doi.org/10.1016/j.ajps.2018.02.004
  • [31]Paarakh MP, Jose PA, Setty CM, Peterchristoper GV. Release kinetics–concepts and applications. Int J Pharm Res Technol. 2018;8(1):12-20. https://doi.org/10.31838/ijprt/08.01.02
  • [32]Panda N, Panda KC, Reddy AV, Reddy GS, Patro LR. Formulation design and in vitro evaluation studies of matrix diffusion controlled glipizide transdermal patch. J Pharm Chem. 2013;4:5.
  • [33]Korsmeyer RW, Peppas NA. Solute and penetrant diffusion in swellable polymers. III. Drug release from glassy poly (HEMA-co-NVP) copolymers. J Control Release. 1984;1(2):89-98. https://doi.org/10.1016/0168-3659%2884%2990001-4
  • [34]Ritger PL, Peppas NA. A simple equation for description of solute release II. Fickian and anomalous release from swellable devices. J Control Release. 1987;5(1):37-42. http://dx.doi.org/10.1016/0168-3659(87)90034-4
  • [35]Chemate S, Anbhule R. Formulation and evaluation of terbinafine hydrochloride film forming emulgel, Int. J. Drug Res. Tech. 2016;6(3): 164-174. https://www.ijdrt.com/articles/formulation-and-evaluation-of-terbinafine-hydrochloride-film-forming-emulgel.pdf

Formulation and evaluation of terbinafine hydrochloride invasomal gel for topical drug delivery

Year 2025, Volume: 29 Issue: 3, 1209 - 1226, 04.06.2025
https://doi.org/10.12991/jrespharm.1694393

Abstract

The primary goal of the research was to develop topical invasomal gel of terbinafine hydrochloride with enhanced permeation and sustained drug release. Invasomes were formulated through a mechanical dispersion technique, employing blends of terpenes (citral and d-limonene) and soya phosphatidylcholine. The optimization process involved assessing parameters such as particle size, zeta potential, poly-dispersibility index (PDI), and entrapment efficacy. The invasomal gel, which underwent optimization, was evaluated for drug content, spreadability, viscosity, in vitro and ex vivo drug release, antifungal activity, and stability in the study. Optimized invasomal batch containing d-limonene (0.3 %) and citral (0.685%) exhibited particle size (95.66 ± 0.49 nm), zeta potential (19.3 ± 0.081 mV), and polydispersity index (PDI) (0.274) and entrapment efficacy (86 ± 0.8165 %). In vitro drug release for optimized invasomes showed that 90 % of drug was released in 158 min with increased permeation of drug through skin. The invasomal gel exhibited 90 % of drug release in 557.9 min indicating sustained drug release.

References

  • [1]Kainz K, Bauer MA, Madeo F, Carmona-Gutierrez D. Fungal infections in humans: The silent crisis. Microbial Cell. 2020;7(6):143–145. https://doi.org/10.15698%2Fmic2020.06.718
  • [2]Charles AJ. Superficial cutaneous fungal infections in tropical countries. Dermatol Ther. 2009;22(6):550–559. https://doi.org/10.1111/j.1529-8019.2009.01276.x
  • [3]Ameen M. Epidemiology of superficial fungal infections. Clin Dermatol. 2010;28(2):197–201. https://doi.org/10.1016/j.clindermatol.2009.12.005
  • [4]Hay R. Superficial fungal infections. Medicine. 2013;41(12):716-718. https://doi.org/10.1016/j.mpmed.2013.09.011
  • [5]Karri VN, Raman SK, Kuppusamy G, Mulukutla S, Ramaswamy S, Malayandi R. Terbinafine hydrochloride loaded nanoemulsion based gel for topical application. J Pharm Investig. 2015;45:79-89. http://dx.doi.org/10.1007/s40005-014-0149-9
  • [6]Loftsson T. Drug stability for pharmaceutical scientists. Academic press; 2014 Jan 25.
  • [7]Shrestha S, Pokhrel S, Sharma S, Manandhar M, Alam I. Formulation and evaluation of topical microemulgel loaded with terbinafine HCl microemulsion. Int J Pharm Sci Res. 2017;26:4716-4723. http://dx.doi.org/10.13040/IJPSR.0975-8232.8 (11).4716-23
  • [8]Alberti I, Kalia YN, Naik A, Bonny JD, Guy RH. In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum. J Control Release. 2001;71(3):319–327. https://doi.org/10.1016/s0168-3659(01)00244-9
  • [9]Balfour JA, Faulds D. Terbinafine: A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial mycoses. Drugs. 1992;43:259-284.https://doi.org/10.2165/00003495-199243020-00010
  • [10]Kazakov PV, Golosov SN. A Simple method for obtaining terbinafine hydrochloride. Pharm Chem J. 2004 ;38(4):206–208. https://doi.org/10.1023/B%3APHAC.0000038420.81588.50
  • [11]Hossain AM, Sil BC, Iliopoulos F, Lever R, Hadgraft J, Lane ME. Preparation, characterisation, and topical delivery of terbinafine. Pharmaceutics. 2019;11(10):548. https://doi.org/10.3390/pharmaceutics11100548
  • [12]Thavva VE, Baratam SR. Formulation and evaluation of terbinafine hydrochloride microsponge gel. Int J Appl Pharm. 2019;11(6):78-85. http://dx.doi.org/10.22159/ijap.2019v11i6.32502
  • [13]Nangare S, Dugam S. Smart invasome synthesis, characterizations, pharmaceutical applications, and pharmacokinetic perspective: a review. Future J Pharm Sci. 2020;6(1):1-21. https://doi.org/10.1186/s43094-020-00145-8
  • [14]Dragicevic-Curic N, Gräfe S, Albrecht V, Fahr A. Topical application of temoporfin-loaded invasomes for photodynamic therapy of subcutaneously implanted tumours in mice: a pilot study. J Photochem Photobiol B: Biology. 2008;91(1):41-50. https://doi.org/10.1016/j.jphotobiol.2008.01.009
  • [15]Zellmer S, Pfeil W, Lasch J. Interaction of phosphatidylcholine liposomes with the human stratum corneum. Biochim Biophys Acta (BBA)-Biomembranes. 1995;1237(2):176-182. https://doi.org/10.1016/0005-2736(95)00100-h
  • [16]Cornwell PA, Barry BW, Bouwstra JA, Gooris GS. Modes of action of terpene penetration enhancers in human skin; differential scanning calorimetry, small-angle X-ray diffraction and enhancer uptake studies. Int J Pharm. 1996;127(1):9-26. https://doi.org/10.1016/0378-5173(95)04108-7
  • [17]Kamran M, Ahad A, Aqil M, Imam SS, Sultana Y, Ali A. Design, formulation and optimization of novel soft nano-carriers for transdermal olmesartan medoxomil delivery: In vitro characterization and in vivo pharmacokinetic assessment. Int J Pharm. 2016;505(1-2):147-158. https://doi.org/10.1016/j.ijpharm.2016.03.030
  • [18]Prasanthi D, K Lakshmi P. Iontophoretic transdermal delivery of finasteride in vesicular invasomal carriers. Pharm Nanotechnol. 2013;1(2):136-150. http://dx.doi.org/10.2174/2211738511301020009
  • [19]Babaie S, Del Bakhshayesh AR, Ha JW, Hamishehkar H, Kim KH. Invasome: A novel nanocarrier for transdermal drug delivery. Nanomaterials. 2020;10(2):341. https://doi.org/10.3390/nano10020341
  • [20]Leite MC, Bezerra AP, Sousa JP, Guerra FQ, Lima ED. Evaluation of antifungal activity and mechanism of action of citral against Candida albicans. Evid-Based Complement Altern Med. 2014: 378280. https://doi.org/10.1155%2F2014%2F378280
  • [21]Han Y, Sun Z, Chen W. Antimicrobial susceptibility and antibacterial mechanism of limonene against Listeria monocytogenes. Molecules. 2019;25(1):33. https://doi.org/10.3390%2Fmolecules25010033
  • [22]Lakshmi PK, Mounica V, Manoj KY, Prasanthi D. Preparation and evaluation of curcumin invasomes. Int J Drug Deliv. 2014;6(2):113. http://www.arjournals.org/index.php/ijdd/index
  • [23]Chaudhari PD, Desai US. Formulation and evaluation of niosomal in situ gel of prednisolone sodium phosphate for ocular drug delivery. Int J Appl Pharm. 2019;97-116. https://doi.org/10.22159/ijap.2019v11i2.30667
  • [24]Mohite R, Mehta P, Arulmozhi S, Kamble R, Pawar A, Bothiraja C. Synthesis of fisetin co-crystals with caffeine and nicotinamide using the cooling crystallization technique: Biopharmaceutical studies. New J Chem. 2019;43(34):13471-13479. https://doi.org/10.1039/C9NJ01848D
  • [25]Kolhe SS. Evaluation of polyherbal ointment for wound healing activity in Wistar rats. J Drug Deliv Ther. 2018;8(6-s):26-31. https://doi.org/10.22270/jddt.v8i6-s.2072
  • [26]Maru AD, Lahoti SR. Formulation and evaluation of ointment containing sunflower wax. Asian J Pharm Clin Res. 2019;12(8):115-120. http://dx.doi.org/10.22159/ajpcr.2019.v12i18.33199
  • [27]Prasad SR, Elango K, Damayanthi D, Saranya JS. Formulation and evaluation of azathioprine loaded silver nanopartilces for the treatment of rheumatoid arthritis. Asian J Biomed Pharm Sci. 2013;3(23):28-32. https://doi.org/10.15272/AJBPS.V3I23.312
  • [28]Alase PP. Sustained ophthalmic delivery of gatifloxacin from in situ gelling system (Doctoral dissertation, Rajiv Gandhi University of Health Sciences (India)). 2006;814–8. http://dx.doi.org/10.4103/0250-474X.31025
  • [29]Satturwar PM, Fulzele SV, Nande VS, Khandare JN. Formulation and evaluation of ketoconazole niosomes. Indian J Pharm Sci. 2002;64(2):155-158.
  • [30]Amnuaikit T, Limsuwan T, Khongkow P, Boonme P. Vesicular carriers containing phenylethyl resorcinol for topical delivery system; liposomes, transfersomes and invasomes. Asian J Pharm Sci. 2018;13(5):472-484. https://doi.org/10.1016/j.ajps.2018.02.004
  • [31]Paarakh MP, Jose PA, Setty CM, Peterchristoper GV. Release kinetics–concepts and applications. Int J Pharm Res Technol. 2018;8(1):12-20. https://doi.org/10.31838/ijprt/08.01.02
  • [32]Panda N, Panda KC, Reddy AV, Reddy GS, Patro LR. Formulation design and in vitro evaluation studies of matrix diffusion controlled glipizide transdermal patch. J Pharm Chem. 2013;4:5.
  • [33]Korsmeyer RW, Peppas NA. Solute and penetrant diffusion in swellable polymers. III. Drug release from glassy poly (HEMA-co-NVP) copolymers. J Control Release. 1984;1(2):89-98. https://doi.org/10.1016/0168-3659%2884%2990001-4
  • [34]Ritger PL, Peppas NA. A simple equation for description of solute release II. Fickian and anomalous release from swellable devices. J Control Release. 1987;5(1):37-42. http://dx.doi.org/10.1016/0168-3659(87)90034-4
  • [35]Chemate S, Anbhule R. Formulation and evaluation of terbinafine hydrochloride film forming emulgel, Int. J. Drug Res. Tech. 2016;6(3): 164-174. https://www.ijdrt.com/articles/formulation-and-evaluation-of-terbinafine-hydrochloride-film-forming-emulgel.pdf
There are 35 citations in total.

Details

Primary Language English
Subjects Pharmacology and Pharmaceutical Sciences (Other)
Journal Section Articles
Authors

Ujwala Desai This is me

Anuradha More This is me

Mayuresh Jadhav This is me

Ganesh Desai This is me

Darshana Wani This is me

Divya Dhamankar This is me

Vishal Vare This is me

Publication Date June 4, 2025
Submission Date February 26, 2024
Acceptance Date August 13, 2024
Published in Issue Year 2025 Volume: 29 Issue: 3

Cite

APA Desai, U., More, A., Jadhav, M., … Desai, G. (2025). Formulation and evaluation of terbinafine hydrochloride invasomal gel for topical drug delivery. Journal of Research in Pharmacy, 29(3), 1209-1226. https://doi.org/10.12991/jrespharm.1694393
AMA Desai U, More A, Jadhav M, et al. Formulation and evaluation of terbinafine hydrochloride invasomal gel for topical drug delivery. J. Res. Pharm. June 2025;29(3):1209-1226. doi:10.12991/jrespharm.1694393
Chicago Desai, Ujwala, Anuradha More, Mayuresh Jadhav, Ganesh Desai, Darshana Wani, Divya Dhamankar, and Vishal Vare. “Formulation and Evaluation of Terbinafine Hydrochloride Invasomal Gel for Topical Drug Delivery”. Journal of Research in Pharmacy 29, no. 3 (June 2025): 1209-26. https://doi.org/10.12991/jrespharm.1694393.
EndNote Desai U, More A, Jadhav M, Desai G, Wani D, Dhamankar D, Vare V (June 1, 2025) Formulation and evaluation of terbinafine hydrochloride invasomal gel for topical drug delivery. Journal of Research in Pharmacy 29 3 1209–1226.
IEEE U. Desai, A. More, M. Jadhav, G. Desai, D. Wani, D. Dhamankar, and V. Vare, “Formulation and evaluation of terbinafine hydrochloride invasomal gel for topical drug delivery”, J. Res. Pharm., vol. 29, no. 3, pp. 1209–1226, 2025, doi: 10.12991/jrespharm.1694393.
ISNAD Desai, Ujwala et al. “Formulation and Evaluation of Terbinafine Hydrochloride Invasomal Gel for Topical Drug Delivery”. Journal of Research in Pharmacy 29/3 (June2025), 1209-1226. https://doi.org/10.12991/jrespharm.1694393.
JAMA Desai U, More A, Jadhav M, Desai G, Wani D, Dhamankar D, Vare V. Formulation and evaluation of terbinafine hydrochloride invasomal gel for topical drug delivery. J. Res. Pharm. 2025;29:1209–1226.
MLA Desai, Ujwala et al. “Formulation and Evaluation of Terbinafine Hydrochloride Invasomal Gel for Topical Drug Delivery”. Journal of Research in Pharmacy, vol. 29, no. 3, 2025, pp. 1209-26, doi:10.12991/jrespharm.1694393.
Vancouver Desai U, More A, Jadhav M, Desai G, Wani D, Dhamankar D, et al. Formulation and evaluation of terbinafine hydrochloride invasomal gel for topical drug delivery. J. Res. Pharm. 2025;29(3):1209-26.