Recent advances in the development of asenapine formulations

References

• Chong HY, Teoh SL, Wu DB-C, et al. Global economic burden of schizophrenia: a systematic review. Neuropsychiatr Dis Treat. 2016;12:357–373.
   PubMed Web of Science ®Google Scholar
• Saha S, Chant D, Welham J, et al. A Systematic Review of the Prevalence of Schizophrenia. PLoS Med. 2005;2(5):e141.
   PubMed Web of Science ®Google Scholar
• Messias EL, Chen C-Y, Eaton WW. Epidemiology of schizophrenia: review of findings and myths. Psychiatr Clin North Am. 2007;30(3):323–338.
   PubMed Web of Science ®Google Scholar
• Stępnicki P, Kondej M, Kaczor AA. Current concepts and treatments of schizophrenia. Molecules. 2018;23(8):2087.
   PubMed Web of Science ®Google Scholar
• Miller BJ, Paschal CB, III DP. Svendsen, mortality and medical comorbidity among patients with serious mental illness. Psychiat Serv. 2006;57(10):1482–1487.
   PubMed Web of Science ®Google Scholar
• Rector NA, Stolar N, Grant P. Schizophrenia: cognitive theory, research, and therapy. New York: Guilford Press; 2011. https://www.guilford.com/books/Schizophrenia/Beck-Rector-Stolar-Grant/9781609182380
   Google Scholar
• Kesby JP, Cui X, Burne THJ, et al. Altered dopamine ontogeny in the developmentally vitamin D deficient rat and its relevance to schizophrenia. Front Cell Neurosci. 2013;7. DOI:10.3389/fncel.2013.00111.
   PubMed Web of Science ®Google Scholar
• Mueser KT, Jeste DV. Clinical handbook of schizophrenia. New York: Guilford Press; 2011.
   Google Scholar
• Remington G, Addington D, Honer W, et al. Guidelines for the pharmacotherapy of schizophrenia in adults. Can J Psychiatry. 2017;62(9):604–616.
   PubMed Web of Science ®Google Scholar
• Grover S, Chakrabarti S, Kulhara P, et al. Clinical practice guidelines for management of schizophrenia. Indian J Psychiatry. 2017;59(5):19–33.
   Web of Science ®Google Scholar
• Keating D, McWilliams S, Schneider I, et al. Pharmacological guidelines for schizophrenia: a systematic review and comparison of recommendations for the first episode. BMJ Open. 2017;7(1):1–10.
   Web of Science ®Google Scholar
• Hasan A, Falkai P, Wobrock T, et al. World federation of societies of biological psychiatry (WFSBP) guidelines for biological treatment of schizophrenia, part 1: update 2012 on the acute treatment of schizophrenia and the management of treatment resistance. World J Biol Psychiatry. 2012;13(5):318–378.
   PubMed Web of Science ®Google Scholar
• World Federation of Societies of Biological Psychiatry (WFSBP). Guidelines for biological treatment of schizophrenia, Part 2: update 2012 on the long-term treatment of schizophrenia and management of antipsychotic-induced side effects. World J Biol Psychiatry. 2013;10:2–44.
   Google Scholar
• Lally J, MacCabe JH. Antipsychotic medication in schizophrenia: a review. Br Med Bull. 2015;114(1):169–179.
   PubMed Web of Science ®Google Scholar
• Solmi M, Murru A, Pacchiarotti I, et al. Safety, tolerability, and risks associated with first-and second-generation antipsychotics: a state-of-the-art clinical review. Ther Clin Risk Manag. 2017;13:757–777.
   PubMed Web of Science ®Google Scholar
• Correll CU. From receptor pharmacology to improved outcomes: individualising the selection, dosing, and switching of antipsychotics. Eur Psychiatry. 2010;25(S2):S12–S21.
   PubMedGoogle Scholar
• Barnes TR. Schizophrenia consensus group of the British association for psychopharmacology. Evidence-based guidelines for the pharmacological treatment of schizophrenia: recommendations from the British Association for Psychopharmacology. J Psychopharmacol. 2011;25(5):567–620.
   PubMed Web of Science ®Google Scholar
• Haddad PM, Brain C, Scott J. Nonadherence with antipsychotic medication in schizophrenia: challenges and management strategies, Patient Relat. Outcome Meas. 2014;5:43–62.
   PubMedGoogle Scholar
• Patel KR, Cherian J, Gohil K, et al. Schizophrenia: overview and treatment options. Pharm Ther. 2014;39: 638–645. PMID: 25210417.
   Google Scholar
• Lewis DA, Lieberman JA. Catching up on schizophrenia: natural history and neurobiology. Neuron. 2000;28(2):325–334.
   PubMed Web of Science ®Google Scholar
• Cortese L, Bressan RA, Castle DJ, et al. Management of schizophrenia: clinical experience with asenapine. J Psychopharmacol. 2013;27(4_suppl):14–22.
   PubMedGoogle Scholar
• Tandon R, Jibson MD. Efficacy of newer generation antipsychotics in the treatment of schizophrenia. Psychoneuroendocrinology. 2003;28:9–26.
   PubMed Web of Science ®Google Scholar
• 022117s022lbl.pdf. n.d.. [cited 2020 Jan 13]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf.
   Google Scholar
• Citrome L. Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism. Expert Opin Drug Metab Toxicol. 2014;10(6):893–903.
   PubMed Web of Science ®Google Scholar
• USFDA, Sycrest, Eur. Med. Agency. 2018. [cited 2020 Apr 5]. https://www.ema.europa.eu/en/medicines/human/EPAR/sycrest.
   Google Scholar
• Balaraman R, Gandhi H. Asenapine, a new sublingual atypical antipsychotic. J Pharmacol Pharmacother. 2010;1(1):60–61. .
   PubMedGoogle Scholar
• Vieta E, Montes JM. A review of asenapine in the treatment of bipolar disorder. Clin Drug Investig. 2018;38(2):87–99.
   PubMed Web of Science ®Google Scholar
• Dogterom P, de Greef R, Peeters PA. The effect of food on the high clearance drug asenapine after sublingual administration to healthy male volunteers. Eur J Clin Pharmacol. 2015;71(1):65–74.
   PubMed Web of Science ®Google Scholar
• Gerrits M, de Greef R, Peeters P. Effect of absorption site on the pharmacokinetics of sublingual asenapine in healthy male subjects. Biopharm Drug Dispos. 2010;31:351–357.
   PubMed Web of Science ®Google Scholar
• van de Wetering-krebbers SF, Jacobs PL, Kemperman GJ, et al. Metabolism and excretion of asenapine in healthy male subjects. Drug Metab Dispos. 2011;39(4):580–590.
   PubMed Web of Science ®Google Scholar
• Citrome L. Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Int J Clin Pract. 2009;63(12):1762–1784.
   PubMed Web of Science ®Google Scholar
• Reynolds GP. Receptor mechanisms of antipsychotic drug action in bipolar disorder–focus on asenapine. Ther Adv Psychopharmacol. 2011;1(6):197–204.
   PubMedGoogle Scholar
• Andrée B, Halldin C, Vrijmoed-de Vries M, et al. Central 5-HT2A and D2 dopamine receptor occupancy after sublingual administration of ORG 5222 in healthy men. Psychopharmacol (Berl). 1997;131(4):339–345.
   PubMed Web of Science ®Google Scholar
• Shahid M, Walker GB, Zorn SH, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol (Oxf). 2009;23(1):65–73.
   PubMed Web of Science ®Google Scholar
• Ghanbari R, El Mansari M, Shahid M, et al. Electrophysiological characterization of the effects of asenapine at 5-HT1A, 5-HT2A, α2-adrenergic and D2 receptors in the rat brain. Eur Neuropsychopharmacol. 2009;19(3):177–187.
   PubMed Web of Science ®Google Scholar
• Potkin SG, Cohen M, Panagides J. Efficacy and tolerability of asenapine in acute schizophrenia: a placebo-and risperidone-controlled trial. J Clin Psychiatry. 2007;68(10):1492–1500.
   PubMed Web of Science ®Google Scholar
• Kane JM, Cohen M, Zhao J, et al. Efficacy and safety of asenapine in a placebo-and haloperidol-controlled trial in patients with acute exacerbation of schizophrenia. J Clin Psychopharmacol. 2010;30(2):106–115.
   PubMed Web of Science ®Google Scholar
• Kinoshita T, Bai Y-M, Kim J-H, et al. Efficacy and safety of asenapine in Asian patients with an acute exacerbation of schizophrenia: a multicentre, randomized, double-blind, 6-week, placebo-controlled study. Psychopharmacology (Berl). 2016;233(14):2663–2674.
   PubMed Web of Science ®Google Scholar
• Kane JM, Mackle M, Snow-Adami L, et al. A randomized placebo-controlled trial of asenapine for the prevention of relapse of schizophrenia after long-term treatment. J Clin Psychiatry. 2011;72(3):349–355.
   PubMed Web of Science ®Google Scholar
• Schoemaker J, Naber D, Vrijland P, et al. Long-term assessment of asenapine vs. olanzapine in patients with schizophrenia or schizoaffective disorder. Pharmacopsychiatry. 2010;43(4):138–146.
   PubMed Web of Science ®Google Scholar
• Schoemaker J, Stet L, Vrijland P, et al. Long-term efficacy and safety of asenapine or olanzapine in patients with schizophrenia or schizoaffective disorder: an extension study. Pharmacopsychiatry. 2012;45(5):196–203.
   PubMed Web of Science ®Google Scholar
• Buchanan RW, Panagides J, Zhao J, et al. Asenapine versus olanzapine in people with persistent negative symptoms of schizophrenia. J Clin Psychopharmacol. 2012;32(1):36–45.
   PubMed Web of Science ®Google Scholar
• Buoli M, Esposito CM, Godio M, et al. Have antipsychotics a different speed of action in the acute treatment of mania? A single-blind comparative study. J Psychopharmacol. 2017;31(12):1537–1543.
   PubMed Web of Science ®Google Scholar
• Casteel M, de Wildt WP, inventors; Organon NV, assignee. Amorphous asenapine and processes for preparing same. United States patent application US 11/868,361. 2008 Apr 17.
   Google Scholar
• Daugherty AL, Mrsny RJ. Transcellular uptake mechanisms of the intestinal epithelial barrier Part one. Pharm Sci Technol Today. 1999;2(4):144–151.
   Google Scholar
• Sharma P, Chawla HPS, Panchagnula R. The role of sorption promoters in increasing the bioavailability of drugs in oral preparations. Drugs Future. 1999;24:1221–1240.
   Google Scholar
• Wessel MD, Jurs PC, Tolan JW, et al. Prediction of human intestinal absorption of drug compounds from molecular structure. J Chem Inf Comput Sci. 1998;38(4):726–735.
   PubMedGoogle Scholar
• Lockman PR, Mumper RJ, Khan MA, et al. Nanoparticle technology for drug delivery across the blood-brain barrier. Drug Dev Ind Pharm. 2002;28(1):1–13.
   PubMed Web of Science ®Google Scholar
• Couvreur P, Vauthier C. Nanotechnology: intelligent design to treat complex disease. Pharm Res. 2006;23(7):1417–1450.
   PubMed Web of Science ®Google Scholar
• Agrawal M, Saraf S, Saraf S, et al. Recent advancements in the field of nanotechnology for the delivery of anti-Alzheimer drug in the brain region. Expert Opin Drug Deliv. 2018;15(6):589–617.
   PubMed Web of Science ®Google Scholar
• Appanna CK, Navya Lakshmi RS, Swathi M. Formulation and characterization of asenapine maleate nanoparticles. Int J Pharm Sci Rev Res. 2016;40:1–5.
   Google Scholar
• Supriya A, Sundaraseelan J, Murthy BS, et al. Formulation and evaluation of capsules of asenapine maleate loaded chitosan nanoparticles. Acta Sci Pharm Sci. 2018;2:29–37.
   Google Scholar
• Lucks JS, Müller RH. Medication vehicles made of solid lipid particles (solid lipid nanospheres SLN), EP0000605497. 1991.
   Google Scholar
• Müller RH, Olbrich C. Neue Adjuvantien in der Impfstofftechnologie. Pharmazeutische Biotechnologie W. Verlagsgesellschaft. Wiss Verlagsgesellschaft Stuttg. 2000;283–302.
   Google Scholar
• Mehnert W, Mäder K. Solid lipid nanoparticles: production, characterization and applications. Adv Drug Deliv Rev. 2012;64:83–101.
   Web of Science ®Google Scholar
• Managuli RS, Wang JT, Faruqu FN, et al. Asenapine maleate-loaded nanostructured lipid carriers: optimization and in vitro, ex vivo and in vivo evaluations. Nanomed. 2019;14(7):889–910.
   PubMed Web of Science ®Google Scholar
• Bhargavi N, Jaimini G, Pranav S, et al. Asenapine maleate loaded solid lipid nanoparticles for oral delivery. Int Res J Pharm. 2017;8(11):45–53.
   Google Scholar
• Sha X, Yan G, Wu Y, et al. Effect of self-microemulsifying drug delivery systems containing Labrasol on tight junctions in Caco-2 cells. Eur J Pharm Sci. 2005;24:477–486.
   PubMed Web of Science ®Google Scholar
• Patel M, Mundada V, Sawant K. Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies. Artif Cells Nanomedicine Biotechnol. 2019;47(1):144–153.
   PubMed Web of Science ®Google Scholar
• Gambhire VM, Ranpise NS. Enhanced oral delivery of asenapine maleate from solid lipid nanoparticles: pharmacokinetic and brain distribution evaluations. Asian J Pharm. 2018;12:152–161.
   Web of Science ®Google Scholar
• Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’drug delivery systems. Eur J Pharm Sci. 2000;11:93–98.
   PubMed Web of Science ®Google Scholar
• Pouton C. Self-emulsifying drug delivery systems: assessment of the efficiency of emulsification. Int J Pharm. 1985;27(2–3):335–348.
   Web of Science ®Google Scholar
• Abdalla A, Klein S, Mäder K. A new self-emulsifying drug delivery system (SEDDS) for poorly soluble drugs: characterization, dissolution, in vitro digestion and incorporation into solid pellets. Eur J Pharm Sci. 2008;35(5):457–464.
   PubMed Web of Science ®Google Scholar
• Patton JS, Carey MC. Watching fat digestion. Science. 1979;204(4389):145–148.
   PubMed Web of Science ®Google Scholar
• Carey MC, Small DM, Bliss CM. Lipid digestion and absorption. Annu Rev Physiol. 1983;45(1):651–677.
   PubMedGoogle Scholar
• Fatouros DG, Deen GR, Arleth L, et al. Structural development of self nano emulsifying drug delivery systems (SNEDDS) during in vitro lipid digestion monitored by small-angle X-ray scattering. Pharm Res. 2007;24(10):1844–1853.
   PubMed Web of Science ®Google Scholar
• Wei L, Sun P, Nie S, et al. Preparation and evaluation of SEDDS and SMEDDS containing carvedilol. Drug Dev Ind Pharm. 2005;31(8):785–794.
   PubMed Web of Science ®Google Scholar
• Hong JY, Kim JK, Song YK, et al. A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption. J Control Release. 2006;110(2):332–338.
   PubMed Web of Science ®Google Scholar
• Arida AI, Al-Tabakha MM, Hamoury HAJ. Improving the high variable bioavailability of griseofulvin by SEDDS. Chem Pharm Bull. 2007;55(12):1713–1719.
   PubMed Web of Science ®Google Scholar
• Patel MH, Mundada VP, Sawant KK. Novel drug delivery approach via self-microemulsifying drug delivery system for enhancing oral bioavailability of asenapine maleate: optimization, characterization, cell uptake, and in vivo pharmacokinetic studies. AAPS PharmSciTech. 2019;20(2):44.
   PubMed Web of Science ®Google Scholar
• Avasarala H, Dinakaran SK, Kakaraparthy R, et al. Self-emulsifying drug delivery system for enhanced solubility of asenapine maleate: design, characterization, in vitro, ex vivo and in vivo appraisal. Drug Dev Ind Pharm. 2019;45(4):548–559.
   PubMed Web of Science ®Google Scholar
• Agrawal M, Ajazuddin, Tripathi DK, et al. Recent advancements in liposomes targeting strategies to cross blood-brain barrier (BBB) for the treatment of Alzheimer’s disease. J Control Release. 2017;260:61–77.
   PubMed Web of Science ®Google Scholar
• Managuli RS, Wang JT-W, Faruqu FM, et al. Surface engineered nanoliposomal platform for selective lymphatic uptake of asenapine maleate: in vitro and in vivo studies. Mater Sci Eng C. 2020;109:1–35.
   Web of Science ®Google Scholar
• Kapadia YD, Sodha HP, Patel VP. Formulation development and evaluation of sublingual film of asenapine maleate. Pharma Sci Monitor. 2013;4:190–209.
   Google Scholar
• Kokare CK, Tagalpallewar AA, Aragade PS, et al. Formulation, evaluation and optimization of asenapine maleate fast mouth dissolving film. J Pharm Sci Pharmacol. 2015;2(3):194–207.
   Google Scholar
• Szejtli J. Cyclodextrin Inclusion Complexes, Cyclodext. Technol. Netherlands, Dordrecht: Springer, 1988:79–185. DOI:10.1007/978-94-015-7797-7_2.
   Google Scholar
• Kulkarni JA, Avachat AM, Avachat CM, et al. Preferential formulation of second generation antipsychotic asenapine as inclusion complex with sulphobutylether-βCD (Captisol): in vitro and In vivo evaluation. Curr Drug Deliv. 2018;15(4):520–531.
   PubMed Web of Science ®Google Scholar
• Patel S, Chavhan S, Soni H, et al. Brain targeting of risperidone-loaded solid lipid nanoparticles by intranasal route. J Drug Target. 2011;19(6):468–474.
   PubMed Web of Science ®Google Scholar
• Kozlovskaya L, Stepensky D. Quantitative analysis of the brain-targeted delivery of drugs and model compounds using nano-delivery systems. J Control Release. 2013;171(1):17–23.
   PubMed Web of Science ®Google Scholar
• Pardeshi CV, Belgamwar VS. Direct nose to brain drug delivery via integrated nerve pathways bypassing the blood–brain barrier: an excellent platform for brain targeting. Expert Opin Drug Deliv. 2013;10(7):957–972.
   PubMed Web of Science ®Google Scholar
• Kulkarni K, Bhambere T, Chaudhary G, et al. Brain targetting through intranasal route. Brain. 2013;5:1441–1450.
   Google Scholar
• Djupesland PG, Messina JC, Mahmoud RA. The nasal approach to delivering treatment for brain diseases: an anatomic, physiologic, and delivery technology overview. Ther Deliv. 2014;5(6):709–733.
   PubMedGoogle Scholar
• Kumar M, Misra A, Babbar AK, et al. Intranasal nanoemulsion based brain targeting drug delivery system of risperidone. Int J Pharm. 2008;358(1–2):285–291.
   PubMed Web of Science ®Google Scholar
• Patel RB, Patel MR, Bhatt KK, et al. Risperidone microemulsion for transnasal delivery: pharmacodynamic and pharmacokinetic evaluation. Pharm Nanotechnol. 2013;1(1):44–53.
   Google Scholar
• Illum L. Nasal drug delivery: problems, possibilities and solutions. J Control Release. 2003;87(1–3):187–198.
   PubMed Web of Science ®Google Scholar
• Alexander A, Saraf S. Nose-to-brain drug delivery approach: A key to easily accessing the brain for the treatment of Alzheimer’s disease. Neural Regen Res. 2018;13(12):2102.
   PubMed Web of Science ®Google Scholar
• Singh SK, Hidau MK, Gautam S, et al. Glycol chitosan functionalized asenapine nanostructured lipid carriers for targeted brain delivery: pharmacokinetic and teratogenic assessment. Int J Biol Macromol. 2018;108:1092–1100.
   PubMed Web of Science ®Google Scholar
• Alexander A, Agrawal M, Saraf S, et al. Chougule, Formulation strategies of nano lipid carrier for effective brain targeting of anti-AD drugs. Curr Pharm Des. 2020;26. DOI:10.2174/1381612826666200212120947.
   PubMed Web of Science ®Google Scholar
• Singh SK, Singh VMR,S. Intranasal delivery of asenapine loaded nanostructured lipid carriers for treatment of schizophrenia. J Nanomedicine Nanotechnol. 2018;12:520–531.
   Google Scholar
• Patel MR, Hirani SN, Patel RB. Microemulsion for nasal delivery of Asenapine maleate in treatment of schizophrenia: formulation considerations. J Pharm Investig. 2018;48(3):301–312.
   Google Scholar
• Alexander A, Agrawal M, Uddin A, et al. Recent expansions of novel strategies towards the drug targeting into the brain. Int J Nanomedicine. 2019;14:5895–5909.
   PubMed Web of Science ®Google Scholar
• Kulkarni JA, Avachat AM. Pharmacodynamic and pharmacokinetic investigation of cyclodextrin-mediated asenapine maleate in situ nasal gel for improved bioavailability. Drug Dev Ind Pharm. 2017;43(2):234–245.
   PubMed Web of Science ®Google Scholar
• Kleiner LW, Wright JC, Wang Y. Evolution of implantable and insertable drug delivery systems. J Control Release. 2014;181:1–10.
   PubMed Web of Science ®Google Scholar
• Avachat AM, Kapure SS. Asenapine maleate in situ forming biodegradable implant: an approach to enhance bioavailability. Int J Pharm. 2014;477(1–2):64–72.
   PubMedGoogle Scholar
• Siegel S, Karen I W, Raquel E G, et al. Surgically implantable long-term antipsychotic delivery systems for the treatment of schizophrenia. Neuropsychopharmacology. 2002;26(6):817–823.
   PubMed Web of Science ®Google Scholar
• Shreya AB, Managuli RS, Menon J, et al. Nano-transfersomal formulations for transdermal delivery of asenapine maleate: in vitro and in vivo performance evaluations. J Liposome Res. 2016;26(3):221–232.
   PubMed Web of Science ®Google Scholar
• Manikkath J, Shenoy GG, Pandey S, et al. Response surface methodology for optimization of ultrasound-assisted transdermal delivery and skin retention of asenapine maleate. J Pharm Innov. 2019;14(4):391–399.
   Web of Science ®Google Scholar
• Carandell LS, Bertran JC, Pascual GF, et al., inventors; Laboratorios Lesvi SL, assignee. Monoclinic crystalline form of asenapine maleate with a specific particle size distribution. United States patent US 9,533,994. 2017 Jan 3.
   Google Scholar
• Katkam S, Polavarapu S, Yaddanapudi VM, et al., inventors; Reddy’s Laboratories Ltd, Reddy’s Laboratories Inc, assignee. Asenapine maleate. United States patent US 8,779,161. 2014 Jul 15.
   Google Scholar
• Bertran A, Terradas J, inventors; Laboratories Lesvi SL, assignee. Stable micronised monoclin form of asenapine maleate and its synthesis. United States patent US 9,505,771. 2016 Nov 29.
   Google Scholar
• Frigoli S, Longoni D, Danelli T, et al., inventors; OLON SpA, assignee. Crystalline salts of asenapine. United States patent US 9,447,109. 2016 Sep 20.
   Google Scholar
• Blatter F, Reichenbächer K, inventors; Sandoz AG, assignee. Crystalline asenapine hydrochloride salt forms. United States patent US 9,303,036. 2016 Apr 5.
   Google Scholar
• Blatter F, Reichenbächer K, inventors; Sandoz AG, assignee. Crystalline salts of Asenapine with organic di-acids and tri-acids. United States patent US 9,169,262. 2015 Oct 27.
   Google Scholar
• Blatter F, Reichenbächer K, inventors; Sandoz AG, assignee. Novel crystalline salts of asenapine. United States patent application US 14/116,098. 2014 Jun 12. Patents that describe the process of enhancing the solubility of asenapine to 24 mg/ml
   Google Scholar
• Ventimiglia G, Barreca G, Magrone D, inventors; Chemo Iberica SA, assignee. Polymorphic forms of asenapine maleate and processes for their preparation. United States patent US 8,933,114. 2015 Jan 13.
   Google Scholar
• Heeres GJ, inventor; Organon NV, assignee. Crystal form of asenapine maleate. United States patent US 7,741,358. 2010 Jun 22.
   Google Scholar
• Mohr P, Rietscher R, Eifler R, et al., inventors; LTS Lohmann Therapie Systeme GmbH and Co KG, assignee. Transdermal therapeutic system containing asenapine and polysiloxane or polyisobutylene. United States patent application US 16/470,322. 2020 Mar 19
   Google Scholar
• Mohr P, Rietscher R, Eifler R, et al., inventors; LTS Lohmann Therapie-Systeme GmbH and Co KG, assignee. Transdermal therapeutic system containing asenapine. United States patent application US 16/445,582. 2019 Nov 7.
   Google Scholar
• Yasukochi T, Sonobe A, Amano S, inventors; Hisamitsu Pharmaceutical Co Inc, assignee. Asenapine-containing patch. United States patent application US 15/745,266. 2019 Jan 3.
   Google Scholar
• Sonobe A, Yasukochi T, inventors; Hisamitsu Pharmaceutical Co Inc, assignee. Method for manufacturing asenapine-containing patch. United States patent application US 15/744,956. 2018 Jul 26.
   Google Scholar
• Faassen WA, Kemperman GJ, van Laarhoven JA, inventors; Merck Sharp, Dohme Corp, assignee. Injectable formulations containing asenapine and method of treatment using same. United States patent US 8,658,687. 2014 Feb 25.
   Google Scholar
• Albayrak C, inventor; ALRISE Biosystems GmbH, assignee. Injectable formulations of asenapine. United States patent application US 15/503,250. 2017 Aug 17.
   Google Scholar
• Gujjar CY, Rallabandi BR, Patwari PS, et al., inventors; Alfred E Tiefenbacher (Gmbh and Co Kg), assignee. Orally disintegrating tablet containing asenapine. United States patent US 9,597,291. 2017 Mar 21.
   Google Scholar
• Patel MR, inventor; Navinta Iii Inc, assignee. Pharmaceutical solution of asenapine for sublingual or buccal use. United States patent US 10,085,971. 2018 Oct 2.
   Google Scholar
• Reddy BP, Khadgapathi P, Rao PS, inventors; Hetero Res Foundation, assignee. Pharmaceutical compositions of asenapine. United States patent application US 15/119,439. 2017 Jan 12.
   Google Scholar
• Blumberg LC, Almarsson Ö, inventors; Alkermes Inc, assignee. Asenapine Prodrugs. United States patent application US 12/978,298. 2011 Jul 7.
   Google Scholar
• van der Sterren JE, van den Heuvel DJ, inventors; Synthon BV, assignee. Intranasal administration of asenapine and pharmaceutical compositions therefor. United States patent application US 12/133,106. 2008 Dec 11.
   Google Scholar
• Saphris® (Asenapine) Sublingual Tablets. [cited 2020 Apr 19]. Available from: https://globalrph.com/drugs/saphris-asenapine-sublingual-tablets/
   Google Scholar
• Li H, Qian ZM. Transferrin/transferrin receptor-mediated drug delivery. Med Res Rev. 2002;22(3):225–250.
   PubMed Web of Science ®Google Scholar
• Ghadiri M, Vasheghani-Farahani E, Atyabi F, et al. Transferrin-conjugated magnetic dextran-spermine nanoparticles for targeted drug transport across blood-brain barrier. J Biomed Mater Res A. 2017;105(10):2851–2864.
   PubMed Web of Science ®Google Scholar
• Chinnala KM, Chinnala KM, Chinnala KM, et al. Development of a novel 3-month drug releasing risperidone microspheres. J Pharm Bioallied Sci. 2015;7(1):37–44.
   PubMed Web of Science ®Google Scholar
• Meltzer HY, Bobo WV, Nuamah IF, et al. Efficacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 6-week, placebo-controlled studies. J Clin Psychiatry. 2008;69(5):817–829.
   PubMed Web of Science ®Google Scholar
• Barakat NS, Elbagory IM, Almurshedi AS. Formulation, release characteristics and bioavailability study of oral monolithic matrix tablets containing carbamazepine. AAPS PharmSciTech. 2008;9(3):931–938.
   PubMed Web of Science ®Google Scholar
• Badshah A, Subhan F, Rauf K, et al. Development of controlled-release matrix tablet of risperidone: influence of methocel®- and Ethocel®-based novel polymeric blend on in vitro drug release and bioavailability. AAPS PharmSciTech. 2011;12(2):525–533.
   PubMed Web of Science ®Google Scholar
• Agrawal M, Saraf S, Saraf S, et al. Recent strategies and advances in the fabrication of nano lipid carriers and their application towards brain targeting. J Control Release. 2020;321:372–415.
   PubMed Web of Science ®Google Scholar