339
Views
15
CrossRef citations to date
0
Altmetric
Research Articles

Intranasal Tadalafil nanoemulsions: formulation, characterization and pharmacodynamic evaluation

, , &
Pages 1083-1094 | Received 05 Aug 2018, Accepted 11 Jun 2019, Published online: 29 Jul 2019

References

  • Abdel Aziz M, Mostafa T, Atta H, Rashed L, Marzouk S, Obaia E, Sabry D, Hassouna A, El ‐Shehaby A, Abdel Aziz A. 2007. Oral phosphodiesterase-5 inhibitors: effect of heme oxygenase inhibition on cGMP signalling in rat cavernous tissue. Andrologia. 39:66–70.
  • Aggarwal N, Goindi S, Khurana R. 2013. Formulation, characterization and evaluation of an optimized microemulsion formulation of griseofulvin for topical application. Colloids Surf B Biointerfaces. 105:158–166.
  • Anderson NR, Gullapalli RP. inventors; Lilly Icos Llc, assignee. 2001 Feb 8. Beta-Carboline pharmaceutical compositions. United States patent US 6,841,167.
  • Badr-Eldin SM, Elkheshen SA, Ghorab MM. 2008. Inclusion complexes of tadalafil with natural and chemically modified beta-cyclodextrins. I: preparation and in-vitro evaluation. Eur J Pharm Biopharm. 70:819–827.
  • Baek JS, Pham CV, Myung CS, Cho CW. 2015. Tadalafil-loaded nanostructured lipid carriers using permeation enhancers. Int J Pharm. 495:701–709.
  • Bahadur S, Pathak K. 2012. Physicochemical and physiological considerations for efficient nose-to-brain targeting. Expert Opin Drug Deliv. 9:19–31.
  • Borhade V, Pathak S, Sharma S, Patravale V. 2012. Clotrimazole nanoemulsion for malaria chemotherapy. Part I: preformulation studies, formulation design and physicochemical evaluation. Int J Pharm. 431:138–148.
  • Bruzziches R, Francomano D, Gareri P, Lenzi A, Aversa A. 2013. An update on pharmacological treatment of erectile dysfunction with phosphodiesterase type 5 inhibitors. Expert Opin Pharmacother. 14:1333–1344.
  • Bshara H, Osman R, Mansour S, El-Shamy A-HA. 2014. Chitosan and cyclodextrin in intranasal microemulsion for improved brain buspirone hydrochloride pharmacokinetics in rats. Carbohydr Polym. 99:297–305.
  • Chapple CR, Roehrborn CG, McVary K, Ilo D, Henneges C, Viktrup L. 2015. Effect of tadalafil on male lower urinary tract symptoms: an integrated analysis of storage and voiding international prostate symptom subscores from four randomised controlled trials. Eur Urol. 67:114–122.
  • Chen L, Staubli SE, Schneider MP, Kessels AG, Ivic S, Bachmann LM, Kessler TM. 2015. Phosphodiesterase 5 inhibitors for the treatment of erectile dysfunction: a trade-off network meta-analysis. Eur Urol. 68:674–680.
  • Cho H-J, Ku W-S, Termsarasab U, Yoon I, Chung C-W, Moon HT, Kim D-D. 2012. Development of udenafil-loaded microemulsions for intranasal delivery: in vitro and in vivo evaluations. Int J Pharm. 423:153–160.
  • Choi H, Kim J, Shim J, Park J, Kang S, Moon D, Cheon J, Lee J, Kim J, Bae J. 2015. Comparison of the efficacy and safety of 5-mg once-daily versus 5-mg alternate-day tadalafil in men with erectile dysfunction and lower urinary tract symptoms. Int J Impot Res. 27:33–37.
  • Constantinides PP. 1995. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm Res. 12:1561–1572.
  • Constantinides PP, Scalart J-P, Lancaster C, Marcello J, Marks G, Ellens H, Smith PL. 1994. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharm Res. 11:1385–1390.
  • Djekic L, Primorac M. 2008. The influence of cosurfactants and oils on the formation of pharmaceutical microemulsions based on PEG-8 caprylic/capric glycerides. Int J Pharm. 352:231–239.
  • Djekic L, Primorac M, Filipic S, Agbaba D. 2012. Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions. Int J Pharm. 433:25–33.
  • Djekic L, Primorac M, Jockovic J. 2011. Phase behaviour, microstructure and ibuprofen solubilization capacity of pseudo-ternary nonionic microemulsions. J Mol Liq. 160:81–87.
  • El-Badry M, Haq N, Fetih G, Shakeel F. 2014a. Measurement and correlation of tadalafil solubility in five pure solvents at (298.15 to 333.15) K. J Chem Eng Data. 59:839–843.
  • El-Badry M, Haq N, Fetih G, Shakeel F. 2014b. Solubility and dissolution enhancement of tadalafil using self-nanoemulsifying drug delivery system. J Oleo Sci. 63:567–576.
  • Elnaggar YS, Etman SM, Abdelmonsif DA, Abdallah OY. 2015. Intranasal piperine‐loaded chitosan nanoparticles as brain‐targeted therapy in Alzheimer’s disease: optimization, biological efficacy, and potential toxicity. J Pharm Sci. 104:3544–3556.
  • Elshafeey AH, Bendas ER, Mohamed OH. 2009. Intranasal microemulsion of sildenafil citrate: in vitro evaluation and in vivo pharmacokinetic study in rabbits. AAPS PharmSciTech. 10:361–367.
  • Fusco F, D’Anzeo G, Sessa A, Pace G, Rossi A, Capece M, d’Emmanuele di Villa Bianca R. 2013. BPH/LUTS and ED: common pharmacological pathways for a common treatment. J Sex Med. 10:2382–2393.
  • Ganta S, Talekar M, Singh A, Coleman TP, Amiji MM. 2014. Nanoemulsions in translational research-opportunities and challenges in targeted cancer therapy. AAPS PharmSciTech. 15:694–708.
  • Gupta M, Kovar A, Meibohm B. 2005. The clinical pharmacokinetics of phosphodiesterase-5 inhibitors for erectile dysfunction. J Clin Pharmacol. 45:987–1003.
  • Hart BL. 1968. Sexual reflexes and mating behavior in the male rat. J Comp Physiol Psychol. 65:453–460.
  • Hatzimouratidis K, Buvat J, Büttner H, Vendeira P, Moncada I, Boehmer M, Henneges C, Boess F. 2014. Psychosocial outcomes after initial treatment of erectile dysfunction with tadalafil once daily, tadalafil on demand or sildenafil citrate on demand: results from a randomized, open-label study. Int J Impot Res. 26:223–229.
  • Hosny KM, Hassan AH. 2014. Intranasal in situ gel loaded with saquinavir mesylate nanosized microemulsion: preparation, characterization, and in vivo evaluation. Int J Pharm. 475:191–197.
  • Huang SA, Lie JD. 2013. Phosphodiesterase-5 (PDE5) inhibitors in the management of erectile dysfunction. P T. 38:407–419.
  • Khafagy E-S, Kamei N, Nielsen EJB, Nishio R, Takeda-Morishita M. 2013. One-month subchronic toxicity study of cell-penetrating peptides for insulin nasal delivery in rats. Eur J Pharm Biopharm. 85:736–743.
  • Kovac JR, DeYoung L, Lehmann KJ, Chung E, Brock GB. 2014. The effects of combined free radical scavenger and sildenafil therapy on age-associated erectile dysfunction: an animal model. Urol Ann. 6:314–320.
  • Kreilgaard M, Pedersen EJ, Jaroszewski JW. 2000. NMR characterisation and transdermal drug delivery potential of microemulsion systems. J Control Release. 69:421–433.
  • Lalani J, Baradia D, Lalani R, Misra A. 2014. Brain targeted intranasal delivery of tramadol: comparative study of microemulsion and nanoemulsion. Pharm Dev Technol. 20:992–1001.
  • Lawrence MJ, Rees GD. 2000. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev. 45:89–121.
  • Laxmi M, Bhardwaj A, Mehta S, Mehta A. 2015. Development and characterization of nanoemulsion as carrier for the enhancement of bioavailability of artemether. Artif Cells Nanomed Biotechnol. 43:334–344.
  • Li Y, Fan X, Li W, Yang P, Zhang H, Tang D, Yin X, Sun J, Zheng A. 2018. Metoclopramide nasal spray in vitro evaluation and in vivo pharmacokinetic studies in dogs. Pharm Dev Technol. 23:275–281.
  • Lowry OH, Rosebrough NJ, Farr AL, Randall RJ. 1951. Protein measurement with the Folin phenol reagent. J Biol Chem. 193:265–275.
  • Lu H-T, Chen R-N, Sheu M-T, Chang C-C, Chou P-Y, Ho H-O. 2011. Rapid-onset sildenafil nasal spray carried by microemulsion systems: in vitro evaluation and in vivo pharmacokinetic studies in rabbits. Xenobiotica. 41:567–577.
  • Mahajan HS, Mahajan MS, Nerkar PP, Agrawal A. 2014. Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting. Drug Deliv. 21:148–154.
  • Malcolmson C, Satra C, Kantaria S, Sidhu A, Lawrence MJ. 1998. Effect of oil on the level of solubilization of testosterone propionate into nonionic oil-in-water microemulsions . J Pharm Sci. 87:109–116.
  • Mehrotra N, Gupta M, Kovar A, Meibohm B. 2007. The role of pharmacokinetics and pharmacodynamics in phosphodiesterase-5 inhibitor therapy. Int J Impot Res. 19:253–264.
  • Obeidat WM, Sallam A-SA. 2014. Evaluation of tadalafil nanosuspensions and their PEG solid dispersion matrices for enhancing its dissolution properties. AAPS PharmSciTech. 15:364–374.
  • Orzechowska BU, Kukowska-Latallo JF, Coulter AD, Szabo Z, Gamian A, Myc A. 2015. Nanoemulsion-based mucosal adjuvant induces apoptosis in human epithelial cells. Vaccine. 33:2289–2296.
  • Paget G, Barnes J. 1964. Toxicity tests. In: Laurence DR, Bacharach AL, editors, Evaluation of drug activities: pharmacometrics. Volume. 1. Berkeley Square, London: Academic Press Inc. Ltd. ; p. 135–166.
  • Patel MR, Patel RB, Bhatt KK, Patel BG, Gaikwad RV. 2016. Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation. Drug Deliv. 23:346–354.
  • Patel RB, Patel MR, Bhatt KK, Patel BG, Gaikwad RV. 2016. Microemulsion-based drug delivery system for transnasal delivery of Carbamazepine: preliminary brain-targeting study. Drug Deliv. 23:207–213.
  • Piao H-M, Balakrishnan P, Cho H-J, Kim H, Kim Y-S, Chung S-J, Shim C-K, Kim D-D. 2010. Preparation and evaluation of fexofenadine microemulsions for intranasal delivery. Int J Pharm. 395:309–316.
  • Prajapati HN, Dalrymple DM, Serajuddin AT. 2012. A comparative evaluation of mono-, di- and triglyceride of medium chain fatty acids by lipid/surfactant/water phase diagram, solubility determination and dispersion testing for application in pharmaceutical dosage form development. Pharm Res. 29:285–305.
  • Shah BM, Misra M, Shishoo CJ, Padh H. 2015. Nose to brain microemulsion-based drug delivery system of rivastigmine: formulation and ex-vivo characterization. Drug Deliv. 22:918–930.
  • Sood S, Jain K, Gowthamarajan K. 2014. Optimization of curcumin nanoemulsion for intranasal delivery using design of experiment and its toxicity assessment. Colloids Surf B Biointerfaces. 113:330–337.
  • Sullivan Jr DW, Gad SC, Julien M. 2014. A review of the nonclinical safety of Transcutol®, a highly purified form of diethylene glycol monoethyl ether (DEGEE) used as a pharmaceutical excipient. Food Chem Toxicol. 72:40–50.
  • Tang SY, Sivakumar M, Ng AM, Shridharan P. 2012. Anti-inflammatory and analgesic activity of novel oral aspirin-loaded nanoemulsion and nano multiple emulsion formulations generated using ultrasound cavitation. Int J Pharm. 430:299–306.
  • Toque HA, Priviero FB, Teixeira CE, Claudino MA, Baracat JS, Fregonesi A, De Nucci G, Antunes E. 2009. Comparative relaxing effects of sildenafil, vardenafil, and tadalafil in human corpus cavernosum: contribution of endogenous nitric oxide release. Urology. 74:216–221.
  • Vinesha V, Sevukarajan M, Rajalakshmi R, Chowdary GT, Haritha K. 2013. Enhancement of solubility of tadalafil by cocrystal approach. Int Res J Pharm. 4:218–223.
  • Washington III SL, Shindel AW. 2010. A once-daily dose of tadalafil for erectile dysfunction: compliance and efficacy. Drug Des Dev Ther. 4:159–171.
  • Wegman A, Windt D, Tulder M, Stalman W, Vries T. 2004. Nonsteroidal antiinflammatory drugs or acetaminophen for osteoarthritis of the hip or knee? A systematic review of evidence and guidelines. J Rheumatol. 31:344–354.
  • Wlodarski K, Sawicki W, Haber K, Knapik J, Wojnarowska Z, Paluch M, Lepek P, Hawelek L, Tajber L. 2015. Physicochemical properties of tadalafil solid dispersions – Impact of polymer on the apparent solubility and dissolution rate of tadalafil. Eur J Pharm Biopharm. 94:106–115.
  • Wlodarski K, Sawicki W, Paluch KJ, Tajber L, Grembecka M, Hawelek L, Wojnarowska Z, Grzybowska K, Talik E, Paluch M. 2014. The influence of amorphization methods on the apparent solubility and dissolution rate of tadalafil. Eur J Pharm Sci. 62:132–140.
  • Zhang P, Liu Y, Feng N, Xu J. 2008. Preparation and evaluation of self-microemulsifying drug delivery system of oridonin. Int J Pharm. 355:269–276.
  • Zhao J, Jitkaew S, Cai Z, Choksi S, Li Q, Luo J, Liu Z-G. 2012. Mixed lineage kinase domain-like is a key receptor interacting protein 3 downstream component of TNF-induced necrosis. Proc Nati Acad Sci USA. 109:5322–5327.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.