Skip to content
2000
image of Sustained Delivery of Dolutegravir Sodium for Better Management of HIV/AIDS via Solid Lipid Nanoparticles

Abstract

Introduction

Human immunodeficiency virus (HIV) is a primary health concern that leads to Acquired immunodeficiency syndrome (AIDS), with more than 39.9 million people living with HIV globally. Dolutegravir sodium is a lipophilic compound with a log P value of 2.2. The current research aimed at augmenting the solubility, dissolution, and therapeutic benefits of Dolutegravir sodium through Solid lipid nanoparticles.

Methods

The solid lipid nanoparticles (SLN) of Dolutegravir sodium were developed using high-speed homogenization and probe sonication methods. The solid lipid and surfactant were scrutinized for the development of SLN. The optimization of SLN was established using the Box-Behnken design model. The effects of lipid, surfactant, and homogenization speed on particle size and entrapment efficiency were evaluated. The colloidal dispersion was lyophilized, and accelerated stability was assessed.

Results

Fourier Transform Infrared Spectroscopy (FTIR) confirmed the interactions between the drug excipients. The thermal behavior and crystalline nature were checked with Differential Scanning Calorimetry (DSC). Among the several tested solid lipids, the highest solubility was observed in glyceryl monostearate (GMS). The colloidal dispersion was stabilized by the Tween 20.

Discussion

Accordingly, the Box-Behnken design model and the analysis of variance (ANOVA) model were applied. The p-values for the particle size and entrapment efficiency were 0.0050 and 0.0010, respectively. The optimized batch D5 showed a particle size of 189 nm, zeta potential (ZP) of -24.6 mV, entrapment efficiency of 85.94%, and drug release of 87.02%. The optimized batch D5 was further lyophilized and analyzed with scanning electron microscopy (SEM), which confirmed the nanoscale range for SLN of Dolutegravir sodium.

Conclusion

A significant enhancement in solubility and dissolution was achieved with the solid lipid nanoparticles. The sustained delivery of 24 hours reduces the dosage frequency and minimizes the viral load for the effective therapy of HIV, thereby improving patients' comfort and compliance.

© 2025 Bentham Science Publishers
Loading

Article metrics loading...

/content/journals/chr/10.2174/011570162X369356250613053801
2025-07-01
2025-09-05

  • From This Site

    /content/journals/chr/10.2174/011570162X369356250613053801
    dcterms_title,dcterms_subject,pub_keyword
    -contentType:Contributor -contentType:Concept -contentType:Institution
    10
    5
Loading full text...

Full text loading...

References

  1. Karim A. Qaisar R. Khalid A. Ahmad F. Hussain M.A. Human immunodeficiency virus/acquired immunodeficiency syndrome knowledge among followers of various religions in India. Asian J Soc Health Behav 2024 7 1 28 36 10.4103/shb.shb_377_23
    [Google Scholar]
  2. Tavelli A Vergori A Cingolani A Orchestra Delphi consen-sus: Clinical management of SARS-CoV-2 infection in people with HIV. Clin Microbiol Infect 2025 S1198-743X (25) 00124 7 10.1016/j.cmi.2025.03.006 40122207
    [Google Scholar]
  3. Visco-Comandini U Burra PTCIA Liver transplantation in people living with HIV: An Italian nationwide survey focusing on hepato-cellular carcinoma and oncologic recurrences Dig Liver Dis 2025 S1590-8658 25 00264 6 10.1016/J.DLD.2025.02.014 40121161
    [Google Scholar]
  4. Pelchen-Matthews A. Mocroft A. Ryom L. Long-term impact of immediate versus deferred antiretroviral therapy on kidney health in people with HIV. Kidney Int. 2024 106 1 136 144 10.1016/j.kint.2024.04.010 38697479
    [Google Scholar]
  5. Choi M.W.Y. Isidoro C.A. Gillgrass A. Mechanisms of mucosal immunity at the female reproductive tract involved in defense against HIV infection. Curr. Opin. Virol. 2024 66 101398 10.1016/j.coviro.2024.101398 38484474
    [Google Scholar]
  6. Naranjo O. Torices S. Clifford P.R. Pericyte infection by HIV-1: A fatal attraction. Retrovirology 2022 19 1 27 10.1186/s12977‑022‑00614‑3 36476484
    [Google Scholar]
  7. Rojas-Celis V. Valiente-Echeverría F. Soto-Rifo R. Toro-Ascuy D. New challenges of HIV-1 infection: How HIV-1 attacks and resides in the central nervous system. Cells 2019 8 10 1245 10.3390/cells8101245 31614895
    [Google Scholar]
  8. Dolutegravir: Uses, interactions, mechanism of action Available from: https://go.drugbank.com/drugs/DB08930
  9. Suárez-García I. Alejos B. Hernando V. Effectiveness and tolerability of dolutegravir/lamivudine for the treatment of HIV-1 infection in clinical practice. J. Antimicrob. Chemother. 2023 78 6 1423 1432 10.1093/jac/dkad102 37099559
    [Google Scholar]
  10. Ashta K.K. Arora S. Khanna R. Raman N. Anilkumar A. Mohan C. A phase-IV non-interventional study to assess virological effectiveness, safety, and tolerability of DTG-based antiretroviral therapy in HIV-1 infected Indian persons living with HIV. Curr. HIV Res. 2024 22 1 31 46 10.2174/011570162X264021231108010324 38284697
    [Google Scholar]
  11. Chu Y. Wong A. Chen H. Development of lipophilic ester prodrugs of dolutegravir for intestinal lymphatic transport. Eur. J. Pharm. Biopharm. 2023 191 90 102 10.1016/j.ejpb.2023.08.015 37634824
    [Google Scholar]
  12. Suthar C. Kanugo A. Liquisolid compact technique for the enhancement of solubility and dissolution rate of ambrisentan: Quality by design approach. Indian J. Pharm. Sci. 2022 84 6 1417 1428 10.36468/pharmaceutical‑sciences.1040
    [Google Scholar]
  13. Kanugo A. Misra A. New and novel approaches for enhancing the oral absorption and bioavailability of protein and peptides therapeutics. 2020 11 11 713 732 10.4155/tde‑2020‑0068
    [Google Scholar]
  14. Mandan J. Kanugo D.A. Recent advancements in nanoparticles-based approaches for the theranostics of glioblastoma multiforme. Curr. Pharm. Biotechnol. 2025 10.2174/0113892010352026250213055117 40108913
    [Google Scholar]
  15. Shewale H. Kanugo A. Formulation optimization and evaluation of patented solid lipid nanoparticles of ambrisentan for pulmonary arterial hypertension. Recent Pat. Nanotechnol. 2024 10.2174/0118722105302631240816115638 39354770
    [Google Scholar]
  16. Zhang L. Mao S. Application of quality by design in the current drug development. Asian J Pharm Sci 2017 12 1 1 8 10.1016/j.ajps.2016.07.006 32104308
    [Google Scholar]
  17. Meravanige G. Ranjitha B.R. Goudanavar P. Design and development of anti-fungal topical gel loaded with solid lipid nanoparticles for wound healing. Ind J Pharm Educ Res 2023 58 1 131 138 10.5530/ijper.58.1.13
    [Google Scholar]
  18. Mulay L. Hegde N. Kanugo A. Formulation optimization and characterization of solid lipid nanoparticles of apixaban. Recent Pat. Nanotechnol. 2025 18 10.2174/0118722105284862240506045944 39099216
    [Google Scholar]
  19. Uner B. Ozdemir S. Tas C. Uner M. Ozsoy Y. Loteprednol-loaded nanoformulations for corneal delivery by quality-by-design concepts: Optimization, characterization, and anti-inflammatory activity. AAPS PharmSciTech 2023 24 4 92 10.1208/s12249‑023‑02551‑6 36977841
    [Google Scholar]
  20. Marinelli L. Dimmito M.P. Cacciatore I. Solid lipid nanoparticles for efficient delivery of capsaicin-rich extract: Potential neuroprotective effects in Parkinson’s disease. J. Drug Deliv. Sci. Technol. 2024 91 105097 10.1016/j.jddst.2023.105097
    [Google Scholar]
  21. Ramadan S.E. El-Gizawy S.A. Osman M.A. Arafa M.F. Application of design of experiment in the optimization of apixaban-loaded solid lipid nanoparticles: In vitro and in vivo evaluation. AAPS PharmSciTech 2023 24 6 167 10.1208/s12249‑023‑02628‑2 37552329
    [Google Scholar]
  22. Kanugo A. Thanvi A. Neusilin US2 based liquisolid Compact technique for the enhancement of solubility and dissolution rate of olmesartan: Box-Behnken design approach. J Res Pharm 2023 27 1 52 66 10.29228/jrp.295
    [Google Scholar]
  23. Wang L. Wang C.Y. Zhang Y. Fu H.J. Gao Y. Zhang K.R. Preparation and characterization of solid lipid nanoparticles loaded with salmon calcitonin phospholipid complex. J. Drug Deliv. Sci. Technol. 2019 52 52 838 845 10.1016/j.jddst.2019.05.045
    [Google Scholar]
  24. Dugad T. Kanugo A. Design optimization and evaluation of solid lipid nanoparticles of azelnidipine for the treatment of hypertension. Recent Pat. Nanotechnol. 2024 18 1 22 32 10.2174/1872210517666221019102543 36278461
    [Google Scholar]
  25. Alhakamy N.A. Hosny K.M. Aldryhim A.Y. Development and optimization of ofloxacin as solid lipid nanoparticles for enhancement of its ocular activity. J. Drug Deliv. Sci. Technol. 2022 72 April 103373 10.1016/j.jddst.2022.103373
    [Google Scholar]
  26. Sharma S. Kanugo A. Gaikwad J. Design and development of solid lipid nanoparticles of tazarotene for the treatment of psoriasis and acne: A quality by design approach. Mater. Technol. 2021 37 8 735 744 10.1080/10667857.2021.1873637
    [Google Scholar]
  27. Akanda M. Mithu M.D.S.H. Douroumis D. Solid lipid nanoparticles: An effective lipid-based technology for cancer treatment. J. Drug Deliv. Sci. Technol. 2023 86 104709 10.1016/j.jddst.2023.104709
    [Google Scholar]
  28. Ayesha B.T. Erum A. Shahid N. Tulain U.R. Saleem U. An effective approach in osteoarthritis: Diacerein-loaded solid lipid nanoparticles, preparation and evaluation for targeted therapy. J. Drug Deliv. Sci. Technol. 2025 108 106856 10.1016/j.jddst.2025.106856
    [Google Scholar]
  29. Mostafaei F. Hemmati S. Valizadeh H. Enhanced intracellular accumulation and cytotoxicity of bortezomib against liver cancer cells using N-stearyl lactobionamide surface modified solid lipid nanoparticles. Int. J. Pharm. 2024 649 123635 10.1016/j.ijpharm.2023.123635 38000649
    [Google Scholar]
  30. Sharma S. Kanugo A. Kaur T. Chaudhary D. Formulation and Characterization of Self-Microemulsifying Drug Delivery System (SMEDDS) of sertraline hydrochloride. Recent Pat. Nanotechnol. 2022 10.2174/1872210516666220623152440 35747954
    [Google Scholar]
  31. Yasir M. Chauhan I. Zafar A. Buspirone loaded solid lipid nanoparticles for amplification of nose to brain efficacy: Formulation development, optimization by Box-Behnken design, in-vitro characterization and in-vivo biological evaluation. J. Drug Deliv. Sci. Technol. 2021 61 61 102164 10.1016/j.jddst.2020.102164
    [Google Scholar]
  32. Kanugo A. Deshpande A. Sharma R. Formulation optimization and evaluation of nanocochleate gel of famciclovir for the treatment of herpes zoster. Recent Pat. Nanotechnol. 2023 17 3 259 269 10.2174/1872210516666220622115553 35733311
    [Google Scholar]
  33. Homayouni Tabrizi M. Soltani M. Es-haghi A. Preparation and characterization of the farnesiferol C-loaded solid lipid nanoparticles decorated with folic acid-bound chitosan and evaluation of its in vitro anti-cancer and anti-angiogenic activities. J. Mol. Liq. 2023 382 121908 10.1016/j.molliq.2023.121908
    [Google Scholar]
  34. Di Costanzo A. Angelico R. Formulation strategies for enhancing the bioavailability of silymarin: The State of the Art. Molecules 2019 24 11 2155 10.3390/molecules24112155 31181687
    [Google Scholar]
  35. Kraisit P. Hirun N. Mahadlek J. Limmatvapirat S. Fluconazole-loaded solid lipid nanoparticles (SLNs) as a potential carrier for buccal drug delivery of oral candidiasis treatment using the Box-Behnken design. J. Drug Deliv. Sci. Technol. 2021 63 63 102437 10.1016/j.jddst.2021.102437
    [Google Scholar]
  36. Trenkenschuh E. Savšek U. Friess W. Formulation, process, and storage strategies for lyophilizates of lipophilic nanoparticulate systems established based on the two models paliperidone palmitate and solid lipid nanoparticles. Int. J. Pharm. 2021 606 July 120929 10.1016/j.ijpharm.2021.120929 34303819
    [Google Scholar]
  37. Khandale N. Birla D. Alam M.S. Quality by design endorsed fabrication of xanthohumol loaded solid nanostructured lipid carrier based powder for effective treatment of Alzheimer’s disease in rats. J. Drug Deliv. Sci. Technol. 2025 107 106792 10.1016/j.jddst.2025.106792
    [Google Scholar]
  38. Ramadan A.E. Elsayed M.M.A. Elsayed A. Development and optimization of vildagliptin solid lipid nanoparticles loaded ocuserts for controlled ocular delivery: A promising approach towards treating diabetic retinopathy. Int. J. Pharm. X 2024 7 100232 10.1016/j.ijpx.2024.100232 38357578
    [Google Scholar]
  39. Mohammadi F. Giti R. Meibodi M.N. Ranjbar A.M. Bazooband A.R. Ramezani V. Preparation and evaluation of kojic acid dipalmitate solid lipid nanoparticles. J. Drug Deliv. Sci. Technol. 2021 61 61 102183 10.1016/j.jddst.2020.102183
    [Google Scholar]
  40. Shahab M.S. Rizwanullah M. Sarim Imam S. Formulation, optimization and evaluation of vitamin E TPGS emulsified dorzolamide solid lipid nanoparticles. J. Drug Deliv. Sci. Technol. 2022 68 68 103062 10.1016/j.jddst.2021.103062
    [Google Scholar]
  41. Uppuluri C.T. Ravi P.R. Dalvi A.V. Design, optimization and pharmacokinetic evaluation of Piribedil loaded solid lipid nanoparticles dispersed in nasal in situ gelling system for effective management of Parkinson’s disease. Int. J. Pharm. 2021 606 July 120881 10.1016/j.ijpharm.2021.120881 34273426
    [Google Scholar]
  42. El-Telbany D.F.A. El-Telbany R.F.A. Zakaria S. Ahmed K.A. El-Feky Y.A. Formulation and assessment of hydroxyzine HCL solid lipid nanoparticles by dual emulsification technique for transdermal delivery. Biomed. Pharmacother. 2021 143 May 112130 10.1016/j.biopha.2021.112130 34560549
    [Google Scholar]
  43. Zaheer Y. Ali M.A. Rehman M. Naringenin loaded solid lipid nanoparticles alleviate oxidative stress and enhance oral bioavailability of naringenin. Colloids Surf. B Biointerfaces 2025 247 114423 10.1016/j.colsurfb.2024.114423 39662145
    [Google Scholar]
  44. Dawoud M. Chitosan coated solid lipid nanoparticles as promising carriers for docetaxel. J. Drug Deliv. Sci. Technol. 2021 62 62 102409 10.1016/j.jddst.2021.102409
    [Google Scholar]
  45. Chettupalli A.K. Unnisa A. Peddapalli H. Jadi R.K. Anusha K. Amarachinta P.R. Development and evaluation of empagliflozin-loaded solid lipid nanoparticles: Pharmacokinetics and pharmacodynamics for oral delivery. Intell Pharm 2025 10.1016/j.ipha.2024.12.004
    [Google Scholar]
/content/journals/chr/10.2174/011570162X369356250613053801
Loading
Sustained Delivery of Dolutegravir Sodium for Better Management of HIV/AIDS via Solid Lipid Nanoparticles
Bentham Science Publishers ; https://doi.org/10.2174/011570162X369356250613053801
/content/journals/chr/10.2174/011570162X369356250613053801
/content/journals/chr/10.2174/011570162X369356250613053801
Loading

Data & Media loading...


  • Article Type:     Research Article
Keywords: Dolutegravir sodium ; nanotechnology in HIV therapy ; HIV ; biopharmaceutical advancements ; solid-lipid nanoparticles ; Box-Behnken design

Most Cited Most Cited RSS feed

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test