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Formulation, design and optimization of antidiabetic drug loaded microspheres

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Abstract

Abstract

The present research aim is to develop the tablet formulation containing microspheres and encapsulating microsphere with antidiabetic drug specially Sitagliptin Phosphate Monohydrate and poly lactic co glycolic acid (PLGA) as a polymer. Preformulation study of the selected drug was carried out. Then, the microspheres were prepared by factorial design, i.e., Design-Expert 12 software (Stat-Ease Inc., USA) was used for designing of experiment, to study interaction between independent variables and dependent variables and deriving optimum formulation. Spray dryer was used for preparation of microspheres. The zeta potential, particle size, infrared spectral analysis, scanning electron microscopy, % drug content, encapsulation efficiency and % drug release were evaluated. Optimized batch F3 showed an average particle size 2500.6 nm. The in vitro drug release at 12th hour and % drug entrapment efficiency of optimized batch F3 was found to be 92.35% and the 34.00%, respectively. The final product has lowered particle size 2500.6 nm and it is focused for well acceptable and suitable due to significant drug release. The final tablet was prepared from optimized batch F3. The precompression parameters, i.e., flow properties of granules, were carried out, and then, post-compression parameters like weight variation, thickness, hardness, friability, % drug content and % drug release were evaluated. The stability study and in vitro antidiabetic study was carried out for tablet. The final product is well acceptable, suitable, palatable, easy for administration and elegant.

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References

  1. Ginter E, Simko V (2012) Type 2 Diabetes mellitus-pandemic in 21st century. Adv Exp Med Biol 771: 42–50. doi: 10.1007/978-1-4614-5441-0_6

  2. Asif AH, Sree H, Puttaswamy NH, Al-Dhubiab B (2018) An effective delivery system of sitagliptin using optimized mucoadhesive nanoparticles. Appl Sci 861:1–13

    Google Scholar 

  3. Kidambi S, Patel SB (2008) Diabetes mellitus considerations for dentistry. J Am Dent Assoc 139:8S-18S

    Article  PubMed  Google Scholar 

  4. Tahrani AA, Bailey CJ, Prato SD, Anthony HB (2011) Management of type 2 diabetes: new and future developments in treatment. The Lancet 378:182–197

    Article  CAS  Google Scholar 

  5. Goldenberg R, Punthakee Z (2013) Definition, classification and diagnosis of diabetes, prediabetes and metabolic syndrome. Can J Diabetes 37:S8–S11

    Article  PubMed  Google Scholar 

  6. Sree H, Attimard M, Khan TA, Nair AB, Aldhubiab BE, Sangi S, Shariff A (2013) Design and formulation of mucoadhesive microspheres of sitagliptin. J Microencapsul 30:257–264

    Article  Google Scholar 

  7. Patel NR, Patel DA, Bharadia PD, Pandya V, Modi D (2011) Microsphere as a novel drug delivery. Int J Pharm Life Sci 2:992–997

    CAS  Google Scholar 

  8. Sanatkar R, Mohammad GRKS, Karimi E, Oskoueian E, Hendra R (2021) Evaluation of daidzein-loaded chitosan microcapsules for the colon cancer drug delivery: synthesis, characterization and release behaviour. Polym Bull. https://doi.org/10.1007/s00289-021-03853-0

    Article  Google Scholar 

  9. Beyrami M, Karimi E, Oskoueian E (2020) Synthesized chrysin-loaded nanoliposomes improves cadmium-induced toxicity in mice. Environ Sci Pollut Res Int 27(32):40643–40651. https://doi.org/10.1007/s11356-020-10113-7

    Article  CAS  PubMed  Google Scholar 

  10. Rahmani F, Karimi E, Oskoueian E (2020) Synthesis and characterisation of chitosan-encapsulated genistein: its anti-proliferative and anti-angiogenic activities. J Microencapsul 37(4):305–313. https://doi.org/10.1080/02652048.2020.1740804

    Article  CAS  PubMed  Google Scholar 

  11. Patil P, Salunkhe V, Bhinge S, Patil S (2021) Formulation optimization and evaluation of glycyrrhetinic acid loaded PLARosome using factorial design: In-vitro anti-ulcer activity. J Indian Chem Soc. https://doi.org/10.1016/j.jics.2021.100199

    Article  Google Scholar 

  12. Vambhurkar GB, Jagatap AM, Gavade AS, Randive DS, Bhutkar MA, Bhinge SD (2021) Formulation and evaluation 0f tablet containing pioglitazone HCL microspheres. J Rep Pharm Sci 10(1):36–41. https://doi.org/10.4103/jrptps.JRPTPS_29_19

    Article  Google Scholar 

  13. Salunkhe VR, Patil PS, Wadkar GH, Bhinge SD (2021) Herbal liposomes: natural network for targeted drug delivery system. J Pharm Res Int 33(29B):31–41

    Article  Google Scholar 

  14. Patil OA, Patil IS, Mane RU, Randive DS, Bhutkar MA, Bhinge SD (2018) Formulation optimization and evaluation of cefdinir nanosuspension using 23 Factorial design. Marmara Pharm J 22(4):587–598. https://doi.org/10.12991/jrp.2018.101

    Article  CAS  Google Scholar 

  15. Akbarzadeh A, Rezaei-Sadabady R, Davaran S, Joo SW, Zarghami N, Hanifehpour Y, Samiei M, Kouhi M, Nejati-Koshki K (2013) Liposome: classification, preparation, and applications. Nanoscale Res Lett 8(1):102. https://doi.org/10.1186/1556-276X-8-102

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  16. Bhattacharya S (2009) Phytosomes: emerging strategy in delivery of herbal drugs and nutraceuticals. Pharma Times 41(3):9–12

    Google Scholar 

  17. Das MK, Ahmed AB, Saha D (2019) Microsphere a drug delivery system–a review. Int J Curr Pharm Res 11(4):34–41

    Article  CAS  Google Scholar 

  18. Kumar A, Mahajan S, Bhandari N (2017) Microspheres: a review. World J Pharm Pharm Sci 6(4):724–740

    CAS  Google Scholar 

  19. Babic A, Vinet L, Chellakudam V, Janikowska K, Allémann E, Lange N (2018) Squalene-PEG-Exendin as high-affinity constructs for pancreatic beta-cell. Bioconjug Chem 29:2531–2540

    Article  CAS  PubMed  Google Scholar 

  20. Smink AM, De Haan BJ, Lakey JRT, De Vos P (2018) Polymer scaffolds for pancreatic islet transplantation-progress and challenges. Am J Transplant 18:2113–2119

    Article  PubMed  Google Scholar 

  21. Vishwakarma G, Pandey SP, Candel HS (2015) Preformulation studies of stavudine for targeted drug delivery system. Int Res J Pharm 6:640–643

    Article  CAS  Google Scholar 

  22. Kala S, Juyal D (2016) Preformulation and characterization studies of aceclofenac active ingredient. J Pharm Innov 5:110–119

    CAS  Google Scholar 

  23. Ravisankar P, Mounika G, Devadasu C, Devala Rao G (2014) A simple validated UV Spectrophotometric method for quantitative analysis of sitagliptin phosphate in pharmaceutical dosage form. J Chem Pharm Sci 7:254–258

    Google Scholar 

  24. Stofella NCF, Veiga A, Oliveira LJ, Montin EF, Andreazza IF (2019) Solid-state characterization of different crystalline forms of sitagliptin. Mater MDPI 12:1–16

    Google Scholar 

  25. Parmar H, Bakliwal S, Gujarathi N, Rane B, Pawar S (2010) Different methods of formulation and evaluation of mucoadhesive microsphere. Int J Appl Biol Pharm 1:1157–1167

    Google Scholar 

  26. Revathi S, Dhanaraju Md (2018) Fabrication and effect of process variables of sitagliptin microspheres. Asian J Pharm Clin Res 11:291–297

    Article  Google Scholar 

  27. Katsarov PD, Pilicheva BA, Manev HM, Lukova PK, Kassarova MI (2017) Optimization of chitosan microspheres spray drying via 32 full factorial design. Folia Med 59:310–317

    Article  CAS  Google Scholar 

  28. Pagar PS, Savkare AD (2017) Formulation and evaluation of omeprazole microspheres by different techniques. Indo Am J Pharm Res 7:426–440

    CAS  Google Scholar 

  29. Kamble MS, Mane OR, Borwandkar VG, Mane SS, Chaudhari PD (2012) Formulation and evaluation of clindamycin HCL–chitosan microspheres for dry powder inhaler formulation. Drug Invent Today 4:527–530

    CAS  Google Scholar 

  30. Vinchurkar K, Mane S, Balekar N, Jain DK (2017) Formulation and evaluation of tablets containing artemether microspheres and lumefantrine. J Drug Deliv Ther 7:4–7

    CAS  Google Scholar 

  31. Lachman L, Herbert AL (1991) The theory and practice of industrial pharmacy. Special Indian 3rd edn, Varghese Publishing House, pp 296–317 (ISBN 0-8121-0977-5)

  32. Malik K, Arora G, Singh I (2011) Taste masked microspheres of ofloxacin: formulation and evaluation of orodispersible tablets. Sci Pharm 79:653–672

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  33. Sangeetha R, Vedasree N (2012) In Vitro α-amylase inhibitory activity of the leaves of thespesia populnea. ISRN Pharmacology 2012:515634. https://doi.org/10.5402/2012/515634

    Article  CAS  PubMed  PubMed Central  Google Scholar 

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Acknowledgements

We express our sincere thanks to Dr. C. S. Magdum, Principal, Rajarambapu College of Pharmacy, Kasegaon, MS—415404, INDIA.

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Authors and Affiliations

  1. Department of Quality Assurance, Rajarambapu College of Pharmacy, Kasegaon, Tal-Walwa, Dist-Sangli, Maharashtra, India

    Tabasum Siraj Mulla & Vijay Rajaram Salunkhe

  2. Shivajirao S Jondhle College of Pharmacy, Asangaon, Thane, Maharashtra, 421601, India

    Nitin Mohire

  3. Department of Pharmaceutical Chemistry, Rajarambapu College of Pharmacy, Tal-Walwa, Dist-Sangli, Maharashtra, 415404, India

    Somnath Devidas Bhinge

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  1. Tabasum Siraj Mulla
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  2. Vijay Rajaram Salunkhe
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  3. Somnath Devidas Bhinge
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Correspondence to Somnath Devidas Bhinge.

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Mulla, T.S., Salunkhe, V.R., Bhinge, S.D. et al. Formulation, design and optimization of antidiabetic drug loaded microspheres. Polym. Bull. 80, 6171–6196 (2023). https://doi.org/10.1007/s00289-022-04325-9

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