Author(s): Atul Tripathi, Amber Vyas

Email(s): ambervyas@gmail.com

DOI: 10.52711/0974-360X.2021.00857   

Address: Atul Tripathi, Amber Vyas*
University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, India.
*Corresponding Author

Published In:   Volume - 14,      Issue - 9,     Year - 2021


ABSTRACT:
Objectives: The aim of the present study was to compare the efficacy of a dual and single drug loaded nano-liposomal formulation of Amphotericin B and Fluconazole for the treatment of visceral leishmaniasis with plain drugs. Methods: We have formulated nano-liposomes (200-250 nm) from Amphotericin B and Fluconazole using dry film hydration method and have tested their efficacy on promastigotes and amastigotes of Leishmania donovani strain. Physicochemical characterization, entrapment study, stability study, in-vitro release study, in-vitro macrophagic uptake studies (Confocal microscopy) and in-vitro antileishmanial activity were evaluated for various formulations containing Amphotericin B and Fluconazole. Results: The in-vitro cellular uptake confocal studies revealed that NR-loaded AmpB + Flu nanoliposomes have enhanced cellular uptake of formulation. The in-vitro inhibition of promastigotes and amastigotes with liposome containing both Amphotericin B and Fluconazole was significantly more than with liposomes containing individual drugs. The IC50 and CC50 of AmpB + Flu nanoliposomes against promastigotes was found to be 3.308µg/mL and 73.48µg/mL respectively, while the IC50 against axenic and intramacrophagic amastigotes was found to be 3.412 and 3.7028µg/mL respectively. Conclusion: In conclusion, Liposomal formulation containing both Amphotericin B and Fluconazole had significantly greater efficacy than conventional combination and other formulation with individual drugs. Current dual drug loaded formulation may have a favourable safety profile, and if production costs are low, it may prove to be a feasible alternative to currently available therapy after in-vivo testing.


Cite this article:
Atul Tripathi, Amber Vyas. In-vitro evaluation of nano-liposomal formulation of Fluconazole and Amphotericin B against visceral leishmaniasis. Research Journal of Pharmacy and Technology. 2021; 14(9):4929-3. doi: 10.52711/0974-360X.2021.00857

Cite(Electronic):
Atul Tripathi, Amber Vyas. In-vitro evaluation of nano-liposomal formulation of Fluconazole and Amphotericin B against visceral leishmaniasis. Research Journal of Pharmacy and Technology. 2021; 14(9):4929-3. doi: 10.52711/0974-360X.2021.00857   Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2021-14-9-71


REFERENCES:
1.    Cazan CD, Pastrav IR, Ionica AM, et al. Updates on the distribution and diversity of sand flies (Diptera: Psychodidae) in Romania. Parasite Vector. 2019;12.
2.    Al-Salem WS, Solorzano C, Weedall GD, et al. Old World cutaneous leishmaniasis treatment response varies depending on parasite species, geographical location and development of secondary infection. Parasite Vector. 2019;12.
3.    Souse SAP, Santos HD, de Carvalho CA, et al. Acute visceral leishmaniasis in a domestic cat (Felis silvestris catus) from the state of Tocantins, Brazil. Semin-Cienc Agrar. 2019;40(4):1723-1729.
4.    Organization WH. Leishmaniasis. WHO Factsheet 2019. 2019.
5.    Organization WH. WHO Technical report Series 949: Control of the leishmaniases. Geneva: WHO. 2010.
6.    Rochelle do Vale Morais A, Silva AL, Cojean S, et al. In-vitro and in-vivo antileishmanial activity of inexpensive Amphotericin B formulations: Heated Amphotericin B and Amphotericin B-loaded microemulsion. Experimental parasitology. 2018; 192:85-92.
7.    Mendonca DVC, Tavares GSV, Lage DP, et al. In vivo antileishmanial efficacy of a naphthoquinone derivate incorporated into a Pluronic (R) F127-based polymeric micelle system against Leishmania amazonensis infection. Biomedicine & Pharmacotherapy. 2019;109:779-787.
8.    Dar MJ, Din FU, Khan GM. Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell. Drug delivery. 2018; 25(1):1595-1606.
9.    Abongomera C, Battaglioli T, Adera C, Ritmeijer K. Severe post-kala-azar dermal leishmaniasis successfully treated with miltefosine in an Ethiopian HIV patient. International Journal of Infectious Diseases. 2019;81:221-224.
10.    Sundar S, Singh A. Chemotherapeutics of visceral leishmaniasis: present and future developments. Parasitology. 2018;145(4):481-489.
11.    Rochelle do Vale Morais A, Silva AL, Cojean S, et al. In-vitro and in-vivo antileishmanial activity of inexpensive Amphotericin B formulations: Heated Amphotericin B and Amphotericin B-loaded microemulsion. Experimental parasitology. 2018;192:85-92.
12.    Abu Ammar A, Nasereddin A, Ereqat S, et al. Amphotericin B-loaded nanoparticles for local treatment of cutaneous leishmaniasis. Drug Delivery and Translational Research. 2019;9(1):76-84.
13.    Koley S, Tiwari N, Neelabh, Singh RK, Singh MS. 2-Mercaptoquinoline Analogues: A Potent Antileishmanial Agent. Chemistryselect. 2018;3(6):1688-1692.
14.    Trinconi CT, Reimao JQ, Yokoyama-Yasunaka JKU, Miguel DC, Uliana SRB. Combination Therapy with Tamoxifen and Amphotericin B in Experimental Cutaneous Leishmaniasis. Antimicrobial agents and chemotherapy. 2014;58(5):2608-2613.
15.    Prates FVD, Dourado MEF, Silva SC, et al. Fluconazole in the Treatment of Cutaneous Leishmaniasis Caused by Leishmania braziliensis: A Randomized Controlled Trial. Clinical Infectious Diseases. 2017;64(1):67-71.
16.    Alrajhi AA, Ibrahim EA, De Vol EB, Khairat M, Faris RM, Maguire JH. Fluconazole for the Treatment of Cutaneous Leishmaniasis Caused byLeishmania major. New Engl J Med. 2002;346(12):891-895.
17.    Sundar S, Chakravarty J. An update on pharmacotherapy for leishmaniasis. Expert opinion on pharmacotherapy. 2015;16(2):237-252.
18.    Sundar S, Chakravarty J. Leishmaniasis: an update of current pharmacotherapy. Expert Opin Pharmacother. 2013;14(1):53-63.
19.    Ortalli M, Varani S, Rosso C, Quintavalla A, Lombardo M, Trombini C. Evaluation of synthetic substituted 1,2-dioxanes as novel agents against human leishmaniasis. European journal of medicinal chemistry. 2019;170:126-140.
20.    Keighobadi M, Emami S, Fakhar M, Shokri A, Mirzaei H, Teshnizi SHJPi. Repurposing azole antifungals into antileishmanials: novel 3-triazolylflavanones with promising in vitro antileishmanial activity against Leishmania major. 2019;69:103-109.
21.    Treiger Borborema SE, Schwendener RA, Osso Junior JA, De Andrade Junior HF, Do Nascimento N. Uptake and antileishmanial activity of meglumine antimoniate-containing liposomes in Leishmania (Leishmania) major-infected macrophages. International journal of antimicrobial agents. 2011; 38(4):341-347.
22.    Sereno D, Lemesre JL. Axenically cultured amastigote forms as an in vitro model for investigation of antileishmanial agents. Antimicrobial agents and chemotherapy. 1997;41(5):972-976.
23.    Shukla AK, Patra S, Dubey VK. Evaluation of selected antitumor agents as subversive substrate and potential inhibitor of trypanothione reductase: an alternative approach for chemotherapy of Leishmaniasis. Mol Cell Biochem. 2011; 352 (1-2): 261-270.
24.    Braga SS. Treating an old disease with new tricks: strategies based on host-guest chemistry for leishmaniasis therapy. J Incl Phenom Macro. 2019;93(3-4):145-155.
25.    Santos JRA, Ribeiro NQ, Bastos RW, et al. High-dose fluconazole in combination with amphotericin B is more efficient than monotherapy in murine model of cryptococcosis. Scientific reports. 2017;7(1):1-8.

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