We use cookies to improve your experience. By continuing to browse this site, you accept our cookie policy.×
Skip main navigation
Aging Health
Bioelectronics in Medicine
Biomarkers in Medicine
Breast Cancer Management
CNS Oncology
Colorectal Cancer
Concussion
Epigenomics
Future Cardiology
Future Medicine AI
Future Microbiology
Future Neurology
Future Oncology
Future Rare Diseases
Future Virology
Hepatic Oncology
HIV Therapy
Immunotherapy
International Journal of Endocrine Oncology
International Journal of Hematologic Oncology
Journal of 3D Printing in Medicine
Lung Cancer Management
Melanoma Management
Nanomedicine
Neurodegenerative Disease Management
Pain Management
Pediatric Health
Personalized Medicine
Pharmacogenomics
Regenerative Medicine
Research Article

Compritol®-based solid lipid nanoparticles of desvenlafaxine prepared by ultrasonication-assisted hot-melt encapsulation to modify its release

    Huma Rao

    *Author for correspondence:

    E-mail Address: huma.rao@iub.edu.pk

    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Punjab, 63100, Pakistan

    ,
    Iqra Rao

    King Edward Medical University Lahore, Lahore, Punjab, Pakistan

    ,
    Saeed Ahmad

    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Punjab, 63100, Pakistan

    ,
    Asadullah Madni

    Department of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Punjab, 63100, Pakistan

    &
    Imtiaz Ahmad

    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Punjab, 63100, Pakistan

    Published Online:https://doi.org/10.2217/nnm-2023-0229

    Aims: Desvenlafaxine (DES) in conventional dosage forms shows initial burst release after oral administration, leading to exaggeration of its side effects. These side effects can be overcome by a sustained-release dosage form using the chemically inert, low-melting-point lipid Compritol® 888 ATO, as it reduces initial burst release. Materials & methods: The potential of DES-loaded solid lipid nanoparticles (DES-SLNs) synthesized by ultrasonication-assisted hot-melt encapsulation to modify the release of DES was investigated. Results: The entrapment efficiency of DES-SLNs was 65.90% with the in vitro release profile showing a sustained-release behavior achieving 81% cumulative release within 16 h without initial burst release. Conclusion: DES-SLNs are a potential carrier for sustained release of water-soluble antidepressant drugs such as DES.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

    References

    • 1. Maeda H. Research spotlight: emergence of EPR effect theory and development of clinical applications for cancer therapy. Ther. Deliv. 5(6), 627–630 (2014).
    • 2. Qushawy M, Nasr A, Abd-Alhaseeb M, Swidan S. Design solid lipid nanoparticles (SLNs) as nano drug delivery carriers: preparation, characterization, and application. Int. J. Appl. Pharm. 12(1), 1–9 (2020). •• Includes discussion of methods and results of solid lipid nanoparticles.
    • 3. Shinde RB, Hosmani AH, Shende MA, Jarag RJ, Thorat YS. Formulation and characterization of solid lipid nanoparticles for an anti-retroviral drug darunavir. Appl. Nanosci. 7(1–2), 47–57 (2017).
    • 4. Kaur IP, Bhandari R, Bhandari S, Kakkar V. Potential of solid lipid nanoparticles in brain targeting. J. Control. Rel. 127(2), 97–109 (2008).
    • 5. Shah M, Agrawal YK, Garala K, Ramkishan A. Solid lipid nanoparticles of a water soluble drug, ciprofloxacin hydrochloride. Indian J. Pharm. Sci. 74(5), 434 (2012).
    • 6. Tong GF, Qin N, Sun LW. Development and evaluation of desvenlafaxine loaded PLGA–chitosan nanoparticles for brain delivery. Saudi Pharm. J. 25(6), 844–851 (2017).
    • 7. Samy W, Elnoby A, El-Gowelli HM, Elgindy N. Hybrid polymeric matrices for oral modified release of desvenlafaxine succinate tablets. Saudi Pharm. J. 25(5), 676–687 (2017).
    • 8. Chakraborty S, Shukla D, Mishra B, Singh S. Lipid – an emerging platform for oral delivery of drugs with poor bioavailability. Eur. J. Pharm. Biopharm. 73(1), 1–15 (2009).
    • 9. Keck C, Ruick R, Müller R. The smartLipids®-3rd generation of lipid nanoparticles after SLN® and NLC® in Controlled Release Society annual meeting. Pharmazie 72(12), 728–735 (2015).
    • 10. Jaspart S, Piel G, Delattre L, Evrard B. Solid lipid microparticles: formulation, preparation, characterisation, drug release and applications. Expert Opin. Drug Deliv. 2(1), 75–87 (2005). • Includes technical aspects of formulation and characterization.
    • 11. Souto EB, Almeida AJ, Müller RH. Lipid nanoparticles (SLN®, NLC®) for cutaneous drug delivery: structure, protection and skin effects. J. Biomed. Nanotechnol. 3(4), 317–331 (2007).
    • 12. Rao H, Ahmad S, Madni A et al. Compritol-based alprazolam solid lipid nanoparticles for sustained release of alprazolam: preparation by hot melt encapsulation. Molecules 27(24), 8894 (2022). •• Includes discussion of methods and results of solid lipid nanoparticles.
    • 13. Emami J, Yousefian H, Sadeghi H. Targeted nanostructured lipid carrier for brain delivery of artemisinin: design, preparation, characterization, optimization and cell toxicity. J. Pharm. Sci. 21(Suppl. 1), S225–S241 (2018). •• Includes discussion of methods and results of solid lipid nanoparticles.
    • 14. Rao H, Ahmad S, Madni A, Ahmad I, Shahzad MN. Single-step extraction for simultaneous quantification of desvenlafaxine and alprazolam in human spiked plasma by RP-HPLC. PLOS ONE 15(9), e0238954 (2020). •• Includes discussion of methods and results of solid lipid nanoparticles.
    • 15. Aslam M, Aqil M, Ahad A et al. Application of Box–Behnken design for preparation of glibenclamide loaded lipid based nanoparticles: optimization, in vitro skin permeation, drug release and in vivo pharmacokinetic study. J. Mol. Liq. 219, 897–908 (2016).
    • 16. Shukla S, Kumar P, Moorthy NS, Shrivastava SK, Trivedi P, Srivastava RS. RP-HPLC method development and its validation for simultaneous estimation of alprazolam and fluoxetine hydrochloride in pharmaceutical dosage form. Eur. J. Anal. Chem. 5(3), 239–245 (2010).
    • 17. Chawla V, Saraf SA. Glyceryl behenate and its suitability for production of aceclofenac solid lipid nanoparticles. JAOCS 88(1), 119–126 (2011).
    • 18. Aburahma MH, Badr-Eldin SM. Compritol 888 ATO: a multifunctional lipid excipient in drug delivery systems and nanopharmaceuticals. Expert Opin. Drug Deliv. 11(12), 1865–1883 (2014).
    • 19. Sivadasan D, Ramakrishnan K, Mahendran J, Ranganathan H, Karuppaiah A, Rahman H. Solid lipid nanoparticles: applications and prospects in cancer treatment. Int. J. Mol. Sci. 24(7), 6199 (2023).
    • 20. Javed S, Mangla B, Almoshari Y, Sultan MH, Ahsan W. Nanostructured lipid carrier system: a compendium of their formulation development approaches, optimization strategies by quality by design, and recent applications in drug delivery. Nanotechnol. Rev. 11(1), 1744–1777 (2022).
    • 21. Hu L, Tang X, Cui F. Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs. J. Pharm. Pharmacol. 56(12), 1527–1535 (2004).
    • 22. Jana S, Maji N, Nayak AK, Sen KK, Basu SK. Development of chitosan-based nanoparticles through inter-polymeric complexation for oral drug delivery. Carbohydr. Polym. 98(1), 870–876 (2013).
    • 23. Najib Ullah SN, Afzal O, Altamimi AS et al. Bedaquiline-loaded solid lipid nanoparticles drug delivery in the management of non-small-cell lung cancer (NSCLC). Pharmaceuticals 16(9), 1309 (2023).
    • 24. Mudalige T, Qu H, Van Haute D, Ansar SM, Paredes A, Ingle T. Characterization of nanomaterials: tools and challenges, in nanomaterials for food applications. In: Nanomaterials for Food Applications Elsevier Inc., MA, USA, 313–353 (2019). •• Includes discussion of methods and results of solid lipid nanoparticles.
    • 25. Rahmanian-Devin P, Askari VR, Sanei-Far Z et al. Preparation and characterization of solid lipid nanoparticles encapsulated noscapine and evaluation of its protective effects against imiquimod-induced psoriasis-like skin lesions. Biomed. Pharmacother. 168, 115823 (2023).
    • 26. Alex A, Paul W, Chacko AJ, Sharma CP. Enhanced delivery of lopinavir to the CNS using Compritol®-based solid lipid nanoparticles. Ther. Deliv. 2(1), 25–35 (2011).
    • 27. Müller RH, Runge SA, Ravelli V, Thünemann AF, Mehnert W, Souto EB. Cyclosporine-loaded solid lipid nanoparticles (SLN®): drug-lipid physicochemical interactions and characterization of drug incorporation. Eur. J. Pharm. Biopharm. 68(3), 535–544 (2008).
    • 28. Duan Y, Dhar A, Patel C et al. A brief review on solid lipid nanoparticles: part and parcel of contemporary drug delivery systems. RSC Adv. 10(45), 26777–26791 (2020).
    • 29. Da Silva JD, de Sousa VP, Cabral LM et al. In vitroin vivo correlation for desvenlafaxine succinate monohydrate extended release tablets. AAPS PharmSciTech 21(5), 1–9 (2020). •• Includes discussion of methods and results of solid lipid nanoparticles.
    • 30. Barzegar-Jalali M. Kinetic analysis of drug release from nanoparticles. J. Pharm. Sci. 11(1), 167–177 (2008).
    • 31. Hogarth C, Arnold K, Wright S, Elkateb H, Rannard S, McDonald TO. Navigating the challenges of lipid nanoparticle formulation: the role of unpegylated lipid surfactants in enhancing drug loading and stability. Nanoscal. Adv. 6(7), 669–679 (2024).
    • 32. Dugad T, Kanugo A. Design optimization and evaluation of solid lipid nanoparticles of azelnidipine for the treatment of hypertension. Recent Pat. Nanotechnol. 18(1), 22–32 (2024).
    • 33. Pareek A, Kothari R, Pareek A et al. Development of a new inhaled swellable microsphere system for the dual delivery of naringenin-loaded solid lipid nanoparticles and doxofylline for the treatment of asthma. Eur. J. Pharm. Sci. 193, 106642 (2024).
    • 34. Khan A, Pawar V, Bagale R, Pendse S, Adapa A. Solid lipid nanoparticles: towards emerging cancer nanomedicine. In: Nanomaterials in Healthcare. CRC Press, Boca Raton, FL, USA, 281–296 (2024).