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Year 2025, Volume: 29 Issue: 4, 1616 - 1626, 05.07.2025
https://doi.org/10.12991/jrespharm.1734545

Abstract

References

  • [1]Midiwo JO, Arot LM. New dialkyl benzoquinones from fruits of Myrsine africana L and Maesalanceolata, Forsk. Nat Prod Lett. 2006; 8(1): 11-14. https://doi.org/10.1080/10575639608043232.
  • [2]Prashanth N, Meghana P, Jain SK, Rajaput PS, Satyanarayan ND, Naika RH. Nicotine promotes epithelial to mesenchymal transition and gemcitabine resistance via hENT1/RRM1 signalling in pancreatic cancer and chemosensitizing effects of Embelin-a naturally occurring benzoquinone. Sci Total Environ. 2024; 914: 169727. https://doi.org/10.1016/j.scitotenv.2023.169727
  • [3]Zafar A, Yasir M, Khalid M, Amir M, Singh L. Pegylated bilosomes for improvement of oral delivery of Biochanin A: Development to preclinical evaluation. S Afr J Bot. 2023; 162: 633-643. https://doi.org/10.1016/j.sajb.2023.09.046.
  • [4]Saifi Z, Rizwanullah M, Mir SR, Amin S. Bilosomes nanocarriers for improved oral bioavailability of acyclovir: A complete characterization through in vitro, ex-vivo and in vivo assessment. J Drug Deliv Sci Technol. 2020; 57: 101634. https://doi.org/10.1016/j.jddst.2020.101634.
  • [5]Ammar HO, Mohamed MI, Tadros MI, Fouly AA. Transdermal Delivery of Ondansetron Hydrochloride via Bilosomal Systems: In Vitro, Ex Vivo, and In Vivo Characterization Studies. AAPS PharmSciTech. 2018;19(5):2276-2287.
  • [6]Dai Y, Zhou R, Liu L, Lu Y, Qi J, Wu W. Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation. Int J Nanomedicine. 2013;8:1921-1933. https://doi.org/10.2147/ijn.s44487.
  • [7]Benson HA. Transdermal drug delivery: penetration enhancement techniques. Curr Drug Deliv. 2005;2(1):23-33. https://doi.org/10.2174/1567201052772915.
  • [8]Tscharnuter W. Photon correlation spectroscopy in particle sizing. In: Tscharnuter W, editor. Encyclopedia of Analytical Chemistry 2000; 5469–5485
  • [9]Singh S, Trivedi S, Jain S. Design and development of proniosome based transdermal delivery of ondansetron hydrochloride. Int J Pharm Biol Res. 2012; 3(5): 191–201.
  • [10]Qushawy M, Soliman GM, Mortagi Y, El-Sherbiny M, Elsherbiny N. Development, optimization, and assessment of losartan nano-bilosomes to mitigate diabetes-induced microvascular complications in sprague dawley rats. J Drug Deliv Sci Technol. 2024; 92:105295. https://doi.org/10.1016/j.jddst.2023.105295.
  • [11]Nallamothu B, Kuche K, Ghadi R, Chaudhari D, Jain S. Enhancing oral bioavailability of insulin through bilosomes: Implication of charge and chain length on apical sodium-dependent bile acid transporter (ASBT) uptake. Int J Biol Macromol. 2023;252:126565. https://doi.org/10.1016/j.ijbiomac.2023.126565.
  • [12]Molinari G, Parlanti P, Aliotta L, Lazzeri A, Gemmi M. TEM morphological analysis of biopolymers: The case of Poly (Lactic Acid) (PLA). Mater Today Commun. 2024; 38: 107868. https://doi.org/10.1016/j.mtcomm.2023.107868
  • [13]Nguyen AN, Messenger KN, Keller LP, Messenger S. Diverse assemblage of presolar and solar system materials in anhydrous interplanetary dust particles: Coordinated NanoSIMS and TEM analyses. Geochim Cosmochim Acta. 2022; 236: 131–149. https://doi.org/10.1016/j.gca.2022.09.005.
  • [14]Christy JV, Balwani A, Mehling H, Agrawal N. Optimization of DSC measurements for organic phase change materials. J Energy Storage. 2023; 73B: 109032. https://doi.org/10.1016/j.est.2023.109032.
  • [15]Tyagi R, Waheed A, Kumar N, Mujeeb M, Naved T, Rashid Khan M, Alhosaini K, Alqarni YA, Rahat R, Alam P, Madan S. In-vitro and ex-vivo antidiabetic, and antioxidant activities of Box-Behnken design optimized Solanum xanthocarpum extract loaded niosomes. Saudi Pharm J. 2023;31(10):101785. https://doi.org/10.1016/j.jsps.2023.101785.
  • [16]Saifi Z, Rizwanullah M, Mir SR, Amin S. Bilosomes nanocarriers for improved oral bioavailability of acyclovir: A complete characterization through in vitro, ex-vivo and in vivo assessment. J Drug Deliv Sci Technol; 2020; 57: 101634. https://doi.org/10.1016/j.jddst.2020.101634.
  • [17]Ammar HO, Mohamed MI, Tadros MI, Fouly AA. Transdermal Delivery of Ondansetron Hydrochloride via Bilosomal Systems: In Vitro, Ex Vivo, and In Vivo Characterization Studies. AAPS PharmSciTech. 2018;19(5):2276-2287. https://doi.org/10.1208/s12249-018-1019-y.
  • [18]Yang H, Liu Z, Song Y, Hu C. Hyaluronic acid-functionalized bilosomes for targeted delivery of tripterine to inflamed area with enhancive therapy on arthritis. Drug Deliv. 2019;26(1):820-830. https://doi.org/10.1080/10717544.2019.1636423
  • [19]Dai Y, Zhou R, Liu L, Lu Y, Qi J. Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation. Int J Nanomedicine. 2013; 8: 1921–1933. https://doi.org/10.2147/ijn.s44487.
  • [20]Felicia LJ, Johnson JC, Philip J. Effect of surfactant on the size, zeta potential and rheology of alumina nanofluids. J Nanofluids. 2014; 3: 328–335. https://doi.org/10.1166/JON.2014.1119.
  • [21]Srikar G, Rani AP. Study on influence of polymer and surfactant on in vitro performance of biodegradable aqueous-core nanocapsules of tenofovirdisoproxil fumarate by response surface methodology. Braz J Pharm Sci. 2019; 55. https://doi.org/10.1590/s2175-97902019000118736.
  • [22]Patel M, Patel N, Patel R. Formulation and evaluation of self-emulsifying drug delivery system of lovastatin. Asian J Pharm Sci. 2010; 5: 266-275.
  • [23]Li J, Yu F, Chen Y, Oupický D. Polymeric drugs: Advances in the development of pharmacologically active polymers. J Control Release.2015; 219: 369–382. https://doi.org/10.1016/j.jconrel.2015.09.043.
  • [24]Parmar K, Patel J, Sheth N. Formulation and optimization of Embelin nanosuspensions using central composite design for dissolution enhancement. Drug Deliv Technol. 2015; 29: 1–7. https://doi.org/10.1016/j.jddst.2015.05.011.
  • [25]Arthanareeswari M, Harshil HD, Ganesh MR, Mohankumar R. Synthesis of Embelin-Fe complex from Embelia ribes fruits and characterization. Materials Today: Proceedings. 2021; 40(Suppl.1): 206–209. https://doi.org/10.1016/j.matpr.2020.10.168
  • [26]Yıldız M. Design, synthesis, characterization, and antimicrobial activity of novel piperazine substituted 1,4-benzoquinones. J. Mol. Struct. 2020; 1203:127422. https://doi.org/10.1016/j.molstruc.2019.127422.
  • [27]Sultan AA, Saad GA, El Maghraby GM. Permeation enhancers loaded bilosomes for improved intestinal absorption and cytotoxic activity of doxorubicin. Int J Pharm. 2023;630:122427. https://doi.org/10.1016/j.ijpharm.2022.122427.

Development and ın vitro characterization of embelin bilosomes for enhanced oral bioavailability

Year 2025, Volume: 29 Issue: 4, 1616 - 1626, 05.07.2025
https://doi.org/10.12991/jrespharm.1734545

Abstract

The goal of this study was to formulate a nanotechnology-based system incorporating surfactants, cholesterol (CHL), and sodium deoxycholate (SDC) and optimization was done using central composite design of design-expert® software. The variables used were X1 (Surfactant; Span 80) and X2 (Bile salt; SDC). In vitro, release kinetics assessment of the drug revealed an increase in drug release of the drug. Transmission electron microscopy (TEM) exhibited a round shape of developed bilosomes with few having rough surfaces. Fourier Transform Infrared Spectroscopy (FT-IR) data exhibited no specific physiochemical interaction between active and additives. Differential scanning calorimetry (DSC) studies showed the molecular state and the indication of no interactions among the formulation ingredients. The mean vesicle size, polydispersity index, zeta potential, and entrapment efficiency (%) of optimized bilosome formulation were observed to be 211.1 nm, 0.513, 47.8 mV, and 99.664 % respectively. Overall, the obtained results confirmed that Embelin-loaded bilosome could be promising for oral drug delivery.

References

  • [1]Midiwo JO, Arot LM. New dialkyl benzoquinones from fruits of Myrsine africana L and Maesalanceolata, Forsk. Nat Prod Lett. 2006; 8(1): 11-14. https://doi.org/10.1080/10575639608043232.
  • [2]Prashanth N, Meghana P, Jain SK, Rajaput PS, Satyanarayan ND, Naika RH. Nicotine promotes epithelial to mesenchymal transition and gemcitabine resistance via hENT1/RRM1 signalling in pancreatic cancer and chemosensitizing effects of Embelin-a naturally occurring benzoquinone. Sci Total Environ. 2024; 914: 169727. https://doi.org/10.1016/j.scitotenv.2023.169727
  • [3]Zafar A, Yasir M, Khalid M, Amir M, Singh L. Pegylated bilosomes for improvement of oral delivery of Biochanin A: Development to preclinical evaluation. S Afr J Bot. 2023; 162: 633-643. https://doi.org/10.1016/j.sajb.2023.09.046.
  • [4]Saifi Z, Rizwanullah M, Mir SR, Amin S. Bilosomes nanocarriers for improved oral bioavailability of acyclovir: A complete characterization through in vitro, ex-vivo and in vivo assessment. J Drug Deliv Sci Technol. 2020; 57: 101634. https://doi.org/10.1016/j.jddst.2020.101634.
  • [5]Ammar HO, Mohamed MI, Tadros MI, Fouly AA. Transdermal Delivery of Ondansetron Hydrochloride via Bilosomal Systems: In Vitro, Ex Vivo, and In Vivo Characterization Studies. AAPS PharmSciTech. 2018;19(5):2276-2287.
  • [6]Dai Y, Zhou R, Liu L, Lu Y, Qi J, Wu W. Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation. Int J Nanomedicine. 2013;8:1921-1933. https://doi.org/10.2147/ijn.s44487.
  • [7]Benson HA. Transdermal drug delivery: penetration enhancement techniques. Curr Drug Deliv. 2005;2(1):23-33. https://doi.org/10.2174/1567201052772915.
  • [8]Tscharnuter W. Photon correlation spectroscopy in particle sizing. In: Tscharnuter W, editor. Encyclopedia of Analytical Chemistry 2000; 5469–5485
  • [9]Singh S, Trivedi S, Jain S. Design and development of proniosome based transdermal delivery of ondansetron hydrochloride. Int J Pharm Biol Res. 2012; 3(5): 191–201.
  • [10]Qushawy M, Soliman GM, Mortagi Y, El-Sherbiny M, Elsherbiny N. Development, optimization, and assessment of losartan nano-bilosomes to mitigate diabetes-induced microvascular complications in sprague dawley rats. J Drug Deliv Sci Technol. 2024; 92:105295. https://doi.org/10.1016/j.jddst.2023.105295.
  • [11]Nallamothu B, Kuche K, Ghadi R, Chaudhari D, Jain S. Enhancing oral bioavailability of insulin through bilosomes: Implication of charge and chain length on apical sodium-dependent bile acid transporter (ASBT) uptake. Int J Biol Macromol. 2023;252:126565. https://doi.org/10.1016/j.ijbiomac.2023.126565.
  • [12]Molinari G, Parlanti P, Aliotta L, Lazzeri A, Gemmi M. TEM morphological analysis of biopolymers: The case of Poly (Lactic Acid) (PLA). Mater Today Commun. 2024; 38: 107868. https://doi.org/10.1016/j.mtcomm.2023.107868
  • [13]Nguyen AN, Messenger KN, Keller LP, Messenger S. Diverse assemblage of presolar and solar system materials in anhydrous interplanetary dust particles: Coordinated NanoSIMS and TEM analyses. Geochim Cosmochim Acta. 2022; 236: 131–149. https://doi.org/10.1016/j.gca.2022.09.005.
  • [14]Christy JV, Balwani A, Mehling H, Agrawal N. Optimization of DSC measurements for organic phase change materials. J Energy Storage. 2023; 73B: 109032. https://doi.org/10.1016/j.est.2023.109032.
  • [15]Tyagi R, Waheed A, Kumar N, Mujeeb M, Naved T, Rashid Khan M, Alhosaini K, Alqarni YA, Rahat R, Alam P, Madan S. In-vitro and ex-vivo antidiabetic, and antioxidant activities of Box-Behnken design optimized Solanum xanthocarpum extract loaded niosomes. Saudi Pharm J. 2023;31(10):101785. https://doi.org/10.1016/j.jsps.2023.101785.
  • [16]Saifi Z, Rizwanullah M, Mir SR, Amin S. Bilosomes nanocarriers for improved oral bioavailability of acyclovir: A complete characterization through in vitro, ex-vivo and in vivo assessment. J Drug Deliv Sci Technol; 2020; 57: 101634. https://doi.org/10.1016/j.jddst.2020.101634.
  • [17]Ammar HO, Mohamed MI, Tadros MI, Fouly AA. Transdermal Delivery of Ondansetron Hydrochloride via Bilosomal Systems: In Vitro, Ex Vivo, and In Vivo Characterization Studies. AAPS PharmSciTech. 2018;19(5):2276-2287. https://doi.org/10.1208/s12249-018-1019-y.
  • [18]Yang H, Liu Z, Song Y, Hu C. Hyaluronic acid-functionalized bilosomes for targeted delivery of tripterine to inflamed area with enhancive therapy on arthritis. Drug Deliv. 2019;26(1):820-830. https://doi.org/10.1080/10717544.2019.1636423
  • [19]Dai Y, Zhou R, Liu L, Lu Y, Qi J. Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation. Int J Nanomedicine. 2013; 8: 1921–1933. https://doi.org/10.2147/ijn.s44487.
  • [20]Felicia LJ, Johnson JC, Philip J. Effect of surfactant on the size, zeta potential and rheology of alumina nanofluids. J Nanofluids. 2014; 3: 328–335. https://doi.org/10.1166/JON.2014.1119.
  • [21]Srikar G, Rani AP. Study on influence of polymer and surfactant on in vitro performance of biodegradable aqueous-core nanocapsules of tenofovirdisoproxil fumarate by response surface methodology. Braz J Pharm Sci. 2019; 55. https://doi.org/10.1590/s2175-97902019000118736.
  • [22]Patel M, Patel N, Patel R. Formulation and evaluation of self-emulsifying drug delivery system of lovastatin. Asian J Pharm Sci. 2010; 5: 266-275.
  • [23]Li J, Yu F, Chen Y, Oupický D. Polymeric drugs: Advances in the development of pharmacologically active polymers. J Control Release.2015; 219: 369–382. https://doi.org/10.1016/j.jconrel.2015.09.043.
  • [24]Parmar K, Patel J, Sheth N. Formulation and optimization of Embelin nanosuspensions using central composite design for dissolution enhancement. Drug Deliv Technol. 2015; 29: 1–7. https://doi.org/10.1016/j.jddst.2015.05.011.
  • [25]Arthanareeswari M, Harshil HD, Ganesh MR, Mohankumar R. Synthesis of Embelin-Fe complex from Embelia ribes fruits and characterization. Materials Today: Proceedings. 2021; 40(Suppl.1): 206–209. https://doi.org/10.1016/j.matpr.2020.10.168
  • [26]Yıldız M. Design, synthesis, characterization, and antimicrobial activity of novel piperazine substituted 1,4-benzoquinones. J. Mol. Struct. 2020; 1203:127422. https://doi.org/10.1016/j.molstruc.2019.127422.
  • [27]Sultan AA, Saad GA, El Maghraby GM. Permeation enhancers loaded bilosomes for improved intestinal absorption and cytotoxic activity of doxorubicin. Int J Pharm. 2023;630:122427. https://doi.org/10.1016/j.ijpharm.2022.122427.
There are 27 citations in total.

Details

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

Shreya Firake This is me

Devanshi Pethani This is me

Jeet Patil This is me

Avinash Bhujbal This is me

Rahul Gondake This is me

Dhanashree Sanap

Sneha Agrawal

Publication Date July 5, 2025
Submission Date April 19, 2024
Acceptance Date September 13, 2024
Published in Issue Year 2025 Volume: 29 Issue: 4

Cite

APA Firake, S., Pethani, D., Patil, J., … Bhujbal, A. (2025). Development and ın vitro characterization of embelin bilosomes for enhanced oral bioavailability. Journal of Research in Pharmacy, 29(4), 1616-1626. https://doi.org/10.12991/jrespharm.1734545
AMA Firake S, Pethani D, Patil J, et al. Development and ın vitro characterization of embelin bilosomes for enhanced oral bioavailability. J. Res. Pharm. July 2025;29(4):1616-1626. doi:10.12991/jrespharm.1734545
Chicago Firake, Shreya, Devanshi Pethani, Jeet Patil, Avinash Bhujbal, Rahul Gondake, Dhanashree Sanap, and Sneha Agrawal. “Development and ın Vitro Characterization of Embelin Bilosomes for Enhanced Oral Bioavailability”. Journal of Research in Pharmacy 29, no. 4 (July 2025): 1616-26. https://doi.org/10.12991/jrespharm.1734545.
EndNote Firake S, Pethani D, Patil J, Bhujbal A, Gondake R, Sanap D, Agrawal S (July 1, 2025) Development and ın vitro characterization of embelin bilosomes for enhanced oral bioavailability. Journal of Research in Pharmacy 29 4 1616–1626.
IEEE S. Firake, D. Pethani, J. Patil, A. Bhujbal, R. Gondake, D. Sanap, and S. Agrawal, “Development and ın vitro characterization of embelin bilosomes for enhanced oral bioavailability”, J. Res. Pharm., vol. 29, no. 4, pp. 1616–1626, 2025, doi: 10.12991/jrespharm.1734545.
ISNAD Firake, Shreya et al. “Development and ın Vitro Characterization of Embelin Bilosomes for Enhanced Oral Bioavailability”. Journal of Research in Pharmacy 29/4 (July2025), 1616-1626. https://doi.org/10.12991/jrespharm.1734545.
JAMA Firake S, Pethani D, Patil J, Bhujbal A, Gondake R, Sanap D, Agrawal S. Development and ın vitro characterization of embelin bilosomes for enhanced oral bioavailability. J. Res. Pharm. 2025;29:1616–1626.
MLA Firake, Shreya et al. “Development and ın Vitro Characterization of Embelin Bilosomes for Enhanced Oral Bioavailability”. Journal of Research in Pharmacy, vol. 29, no. 4, 2025, pp. 1616-2, doi:10.12991/jrespharm.1734545.
Vancouver Firake S, Pethani D, Patil J, Bhujbal A, Gondake R, Sanap D, et al. Development and ın vitro characterization of embelin bilosomes for enhanced oral bioavailability. J. Res. Pharm. 2025;29(4):1616-2.