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2000
Volume 14, Issue 6
  • ISSN: 2210-6812
  • E-ISSN: 2210-6820

Abstract

Aims

The aim of the present study is to formulate and evaluate the Salvia miltorrhiza-loaded Nano-structured lipid carriers (SM-NLC) in order to enhance the aqueous solubility and bioavailability as the efficacy of extract has been restricted due to less solubility and low bioavailability.

Introduction

is a well-known Chinese herb that belongs to the family Labiatae. The herb has been widely used to treat various kinds of ailments, and its main phytochemical constituents are Tanshinone I, Tanshinone II, Miltirone, and Salvionolic acid, which are mainly found in the extract of roots. These Phytochemical constituents are responsible for several pharmacological activities such as anti-oxidant, anti-microbial, anti-hyperlipidemic, anti-inflammatory, cardiovascular diseases .

Objective

Nano-lipid carriers are useful in enhancing the solubility of poor water-soluble drugs. The faulty lattice arrangement of Nano-lipid carriers (NLC) provides better entrapment, thus providing more space for the drug to incorporate in the lattice structure of NLC, improving the stability of the formulation and preventing the drug leakage from the matrix.

Methods

SM-NLCs were prepared by using oleic acid and stearic acid as liquid and solid lipids, respectively and tween 80 as the surfactant by high-speed homogenization method. The optimization of SM- NLC was performed by applying the Box-Behnken experimental design. The independent variables were chosen as the amount of lipids, surfactant concentration, and sonication time, whereas dependent variables were opted as particle size and entrapment efficiency. The influence of different proportions of the lipids (Stearic acid and Oleic acid) and the surfactant (Tween 80) was analysed on the dependent variables. The optimized formulation was evaluated for Particle size (241.7nm±3), Polydispersity index (.249 ±0.05), Zeta Potential (-14.6±5), and entrapment efficiency (82.49%). Scanning Electron Microscopy (SEM) was performed to identify the surface morphology, and the entrapment of the drug into the nanostructured matrix was verified by Differential Scanning Calorimetry. The interaction between the formulations was confirmed by performing FTIR. The dialysis bag method was performed to calculate the drug release from the optimized formulation. Additionally, a stability study was performed for 1 month of duration.

Results

The SM NLCs were successfully formulated based on the Box-Behnken design. Particle size, PDI, zeta potential, and EE demonstrated less than a 5% difference compared to the predicted value. The formulations did not show any possible interactions with the lipids. The optimized formulations were found stable after one month of stability studies.

Conclusion

The above results confirmed that could be effectively formulated in the form of a nanostructured-lipid carrier system. The formulation and evaluation of nanoparticles have been performed successfully using the homogenization method.

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References

  1. El-NewaryS.A. The hypolipidemic effect of Portulaca oleracea L. stem on hyperlipidemic Wister Albino rats.Ann. Agric. Sci.201661111112410.1016/j.aoas.2016.01.002
    [Google Scholar]
  2. FidèleN. JosephB. EmmanuelT. ThéophileD. Hypolipidemic, antioxidant and anti-atherosclerogenic effect of aqueous extract leaves of Cassia occidentalis Linn (Caesalpiniaceae) in diet-induced hypercholesterolemic rats.BMC Complement. Altern. Med.20171717610.1186/s12906‑017‑1566‑x 28122565
    [Google Scholar]
  3. ImamB. The potency of wound healing of nanogel-containing mikania micrantha leaves extract in hyperglycemic rats.Pharm. Nanotechnol.20219533934610.2174/2211738509666211209164105
    [Google Scholar]
  4. Shweta AkhaniS. Hypolipidemic effect of Bacopa monnieri (Brahmi) and Terminalia arjuna (Arjuna): An in vitro study.Natl. J. Physiol. Pharm. Pharmacol.20231351088109110.5455/njppp.2023.13.1154220220804202
    [Google Scholar]
  5. BikiarisD. KaravelidisV. KaravasE. Novel biodegradable polyesters. Synthesis and application as drug carriers for the preparation of raloxifene HCl loaded nanoparticles.Molecules20091472410243010.3390/molecules14072410 19633613
    [Google Scholar]
  6. ZhangW. HeH. WangH. WangS. LiX. LiuY. JiangH. JiangH. YanY. WangY. LiuX. Activation of transsulfuration pathway by salvianolic acid a treatment: A homocysteine-lowering approach with beneficial effects on redox homeostasis in high-fat diet-induced hyperlipidemic rats.Nutr. Metab. (Lond.)20131016810.1186/1743‑7075‑10‑68 24314320
    [Google Scholar]
  7. BaoYi. Wang, Li Salvianolic acid B inhibits macrophage uptake of modified low density lipoprotein (mLDL) in a scavenger receptor CD36-dependent manner.Atherosclerosis2012223115215910.1016/j.atherosclerosis.2012.05.006
    [Google Scholar]
  8. YuH. SubediR.K. NepalP.R. KimY.G. ChoiH.K. Enhancement of solubility and dissolution rate of cryptotanshinone, tanshinone I and tanshinone IIA extracted from Salvia miltiorrhiza.Arch. Pharm. Res.20123581457146410.1007/s12272‑012‑0816‑1 22941489
    [Google Scholar]
  9. NaseriN. ValizadehH. Zakeri-MilaniP. Solid lipid nanoparticles and nanostructured lipid carriers: Structure, preparation and application.Adv. Pharm. Bull.20155330531310.15171/apb.2015.043 26504751
    [Google Scholar]
  10. AlexanderA. AgrawalM. SarafS. SarafS. Ajazuddin; Chougule, M.B. Formulation strategies of nano lipid carrier for effective brain targeting of anti-AD drugs.Curr. Pharm. Des.202026273269328010.2174/1381612826666200212120947 32048957
    [Google Scholar]
  11. SilvaP. BonifácioB. RamosM. NegriK. Maria BauabT. ChorilliM. Nanotechnology-based drug delivery systems and herbal medicines: A review.Int. J. Nanomedicine2013911510.2147/IJN.S52634 24363556
    [Google Scholar]
  12. GhoshV. SaranyaS. MukherjeeA. ChandrasekaranN. Cinnamon oil nanoemulsion formulation by ultrasonic emulsification: Investigation of its bactericidal activity.J. Nanosci. Nanotechnol.201313111412210.1166/jnn.2013.6701 23646705
    [Google Scholar]
  13. KanojiaS.N. GuptaN.N. SinghS. Applications of nanostructured lipid carriers: Recent advancements and patent review.Biointerface Res. Appl. Chem.202112163865210.33263/BRIAC121.638652
    [Google Scholar]
  14. SelvarajK. GowthamarajanK. KarriV.V.S.R. Nose to brain transport pathways an overview: Potential of nanostructured lipid carriers in nose to brain targeting.Artif. Cells Nanomed. Biotechnol.20174681810.1080/21691401.2017.1420073 29282995
    [Google Scholar]
  15. ChatzitakiA.T. JesusS. KaravasiliC. AndreadisD. FatourosD.G. BorgesO. Chitosan-coated PLGA nanoparticles for the nasal delivery of ropinirole hydrochloride: In vitro and ex vivo evaluation of efficacy and safety.Int. J. Pharm.202058911977610.1016/j.ijpharm.2020.119776 32818538
    [Google Scholar]
  16. KapoorH. AqilM. ImamS.S. SultanaY. AliA. Formulation of amlodipine nano lipid carrier: Formulation design, physicochemical and transdermal absorption investigation.J. Drug Deliv. Sci. Technol.20194920921810.1016/j.jddst.2018.11.004
    [Google Scholar]
  17. AgrawalM. SarafS. PradhanM. PatelR.J. SinghviG. Ajazuddin; Alexander, A. Design and optimization of curcumin loaded nano lipid carrier system using Box-Behnken design.Biomed. Pharmacother.202114111191910.1016/j.biopha.2021.111919 34328108
    [Google Scholar]
  18. MohantyD. Development of atomoxetine-loaded nlc in situ gel for nose-to-brain delivery: Optimization, in vitro , and preclinical evaluation.Pharmaceutics2023157198510.3390/pharmaceutics15071985
    [Google Scholar]
  19. AnandA. AryaM. KaithwasG. SinghG. SarafS.A. Sucrose stearate as a biosurfactant for development of rivastigmine containing nanostructured lipid carriers and assessment of its activity against dementia in C. elegans model.J. Drug Deliv. Sci. Technol.20194921922610.1016/j.jddst.2018.11.021
    [Google Scholar]
  20. López-GarcíaR. Ganem-RonderoA. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC): Occlusive effect and penetration enhancement ability.JCDSA201552627210.4236/jcdsa.2015.52008
    [Google Scholar]
  21. Mohammadi-SamaniS. ZojajiS. Entezar-AlmahdiE. Piroxicam loaded solid lipid nanoparticles for topical delivery: Preparation, characterization and in vitro permeation assessment.J. Drug Deliv. Sci. Technol.20184742743310.1016/j.jddst.2018.07.015
    [Google Scholar]
  22. SeoCS. Determination of the marker compound, chikusetsusaponin IVa in Dolichos lablab L. using HPLC–PDA and HPLC–ELSD.S. Afr. J. Bot.202013047147410.1016/j.sajb.2020.01.043
    [Google Scholar]
  23. TummalaS. GowthamarajanK. Satish KumarM.N. PraveenT.K. YamjalaK. TripuraneniN.S. PrakashA. Formulation and optimization of oxaliplatin immuno-nanoparticles using Box–Behnken design and cytotoxicity assessment for synergistic and receptor-mediated targeting in the treatment of colorectal cancer.Artif. Cells Nanomed. Biotechnol.20164481835185010.3109/21691401.2015.1111226 26697734
    [Google Scholar]
  24. CostaC.P. MoreiraJ.N. Sousa Lobo J.M.; Silva, A.C. Intranasal delivery of nanostructured lipid carriers, solid lipid nanoparticles and nanoemulsions: A current overview of in vivo studies.Acta Pharm. Sin. B202111492594010.1016/j.apsb.2021.02.012 33996407
    [Google Scholar]
  25. RajputA.P. ButaniS.B. Resveratrol anchored nanostructured lipid carrier loaded in situ gel via nasal route: Formulation, optimization and in vivo characterization.J. Drug Deliv. Sci. Technol.20195121422310.1016/j.jddst.2019.01.040
    [Google Scholar]
  26. SwapnilS. Patravale docetaxel loaded pomegranate seed oil based nanostructured lipid carriers: A potential alternative to current formulation.AAPS PharmSciTech20202129510.1208/s12249‑020‑01839‑1
    [Google Scholar]
  27. KimM.H. KimK.T. SohnS.Y. LeeJ.Y. LeeC.H. YangH. LeeB.K. LeeK.W. KimD.D. Formulation and evaluation of nanostructured lipid carriers (NLCs) Of 20(S)-protopanaxadiol (PPD) by box-behnken design.Int. J. Nanomedicine2019148509852010.2147/IJN.S215835 31749618
    [Google Scholar]
  28. RayanneR. Ucuùba (Virola surinamensis) fat-based nanostructured lipid carriers for nail drug delivery of ketoconazole: Development and optimization using box-behnken design.Pharmaceutics201911s628410.3390/pharmaceutics11060284
    [Google Scholar]
  29. KharkarP.B. TalkarS.S. PatravaleV.B. A rapid and sensitive bioanalytical rp-hplc method for detection of docetaxel: Developmentand validation.IJPER2017514ss729s73410.5530/ijper.51.4s.105
    [Google Scholar]
  30. LiX. WangD. ZhangJ. PanW. Preparation and pharmacokinetics of docetaxel based on nanostructured lipid carriers.J. Pharm. Pharmacol.200961111485149210.1211/jpp/61.11.0007
    [Google Scholar]
  31. Brito RajS. LavanyaP. Formulation and in-vitro evaluation of acyclovir solid lipid nanoparticles.Int. J. Pharm. Sci. Res.201561495610.13040/IJPSR.0975‑8232.6(1).442‑52
    [Google Scholar]
  32. EatonM.A.W. LevyL. FontaineO.M.A. Delivering nanomedicines to patients: A practical guide.Nanomedicine 201511498399210.1016/j.nano.2015.02.004 25724929
    [Google Scholar]
  33. Garrastazu PereiraG. RawlingT. PozzoliM. PazderkaC. ChenY. DunstanC.R. MurrayM. SonvicoF. Nanoemulsion-enabled oral delivery of novel anticancer ω-3 fatty acid derivatives.Nanomaterials 201881082510.3390/nano8100825 30322115
    [Google Scholar]
  34. UnerM. DamgaliS. OzdemirS. CelikB. Therapeutic potential of drug delivery by means of lipid nanoparticles: Reality or illusion?Curr. Pharm. Des.201823436573659110.2174/1381612823666171122110638 29173153
    [Google Scholar]
  35. RossiI. SonvicoF. McConvilleJ.T. RossiF. FröhlichE. ZellnitzS. RossiA. Del FaveroE. BettiniR. ButtiniF. Nebulized coenzyme Q 10 nanosuspensions: A versatile approach for pulmonary antioxidant therapy.Eur. J. Pharm. Sci.201811315917010.1016/j.ejps.2017.10.024 29066385
    [Google Scholar]
  36. Sánchez-LópezE. EspinaM. DoktorovovaS. SoutoE.B. GarcíaM.L. Lipid nanoparticles (SLN, NLC): Overcoming the anatomical and physiological barriers of the eye – Part II - Ocular drug-loaded lipid nanoparticles.Eur. J. Pharm. Biopharm.2017110586910.1016/j.ejpb.2016.10.013 27789359
    [Google Scholar]
  37. ComfortC. GarrastazuG. PozzoliM. SonvicoF. Opportunities and challenges for the nasal administration of nanoemulsions.Curr. Top. Med. Chem.201515435636810.2174/1568026615666150108144655 25579345
    [Google Scholar]
  38. MüllerR.H. ShegokarR. KeckC.M. 20 years of lipid nanoparticles (SLN and NLC): Present state of development and industrial applications.Curr. Drug Discov. Technol.20118320722710.2174/157016311796799062 21291409
    [Google Scholar]
  39. AgyralidesG.G. DallasP.P. RekkasD.M. Development and in vitro evaluation of furosemide transdermal formulations using experimental design techniques.Int. J. Pharm.20042811-2354310.1016/j.ijpharm.2004.05.011 15288341
    [Google Scholar]
  40. PradhanM. SinghD. MurthyS.N. SinghM.R. Design, characterization and skin permeating potential of Fluocinolone acetonide loaded nanostructured lipid carriers for topical treatment of psoriasis.Steroids2015101566310.1016/j.steroids.2015.05.012 26049018
    [Google Scholar]
  41. MehmoodT. AhmadA. AhmedA. AhmedZ. Optimization of olive oil based O/W nanoemulsions prepared through ultrasonic homogenization: A response surface methodology approach.Food Chem.201722979079610.1016/j.foodchem.2017.03.023 28372245
    [Google Scholar]
  42. AndradeL.M. de Fátima ReisC. Maione-SilvaL. AnjosJ.L.V. AlonsoA. SerpaR.C. MarretoR.N. LimaE.M. TaveiraS.F. Impact of lipid dynamic behavior on physical stability, in vitro release and skin permeation of genistein-loaded lipid nanoparticles.Eur. J. Pharm. Biopharm.2014881404710.1016/j.ejpb.2014.04.015 24816130
    [Google Scholar]
  43. AgrawalM. SarafS. SarafS. DubeyS.K. PuriA. PatelR.J. AjazuddinV. RavichandiranV. MurtyU.S. AlexanderA. Recent strategies and advances in the fabrication of nano lipid carriers and their application towards brain targeting.J. Control. Release202032137241510.1016/j.jconrel.2020.02.020 32061621
    [Google Scholar]
  44. AnwarM. WarsiM.H. MallickN. AkhterS. GahoiS. JainG.K. TalegaonkarS. AhmadF.J. KharR.K. Enhanced bioavailability of nano-sized chitosan–atorvastatin conjugate after oral administration to rats.Eur. J. Pharm. Sci.201144324124910.1016/j.ejps.2011.08.001 21864678
    [Google Scholar]
  45. HeY. LuoL. LiangS. LongM. XuH. Influence of probe-sonication process on drug entrapment efficiency of liposomes loaded with a hydrophobic drug.Int. J. Polym. Mater.201968419319710.1080/00914037.2018.1434651
    [Google Scholar]
  46. CheongA.M. TanC.P. NyamK.L. Physicochemical, oxidative and anti-oxidant stabilities of kenaf seed oil-in-water nanoemulsions under different storage temperatures.Ind. Crops Prod.20179537438210.1016/j.indcrop.2016.10.047
    [Google Scholar]
  47. KhanA. ImamS.S. AqilM. AhadA. SultanaY. AliA. KhanK. Brain targeting of temozolomide via the intranasal route using lipid-based nanoparticles: brain pharmacokinetic and scintigraphic analyses.Mol. Pharm.201613113773378210.1021/acs.molpharmaceut.6b00586 27661966
    [Google Scholar]
  48. SalunkheS.S. BhatiaN.M. BhatiaM.S. Implications of formulation design on lipid-based nanostructured carrier system for drug delivery to brain.Drug Deliv.20162341306131610.3109/10717544.2014.943337 25080227
    [Google Scholar]
  49. GadhaveD. ChoudhuryH. KokareC. Neutropenia and leukopenia protective intranasal olanzapine-loaded lipid-based nanocarriers engineered for brain delivery.Appl. Nanosci.20199215116810.1007/s13204‑018‑0909‑3
    [Google Scholar]
  50. GabalY.M. KamelA.O. SammourO.A. ElshafeeyA.H. Effect of surface charge on the brain delivery of nanostructured lipid carriers in situ gels via the nasal route.Int. J. Pharm.20144731-244245710.1016/j.ijpharm.2014.07.025 25062866
    [Google Scholar]
  51. MengF. AsgharS. XuY. WangJ. JinX. WangZ. WangJ. PingQ. ZhouJ. XiaoY. Design and evaluation of lipoprotein resembling curcumin-encapsulated protein-free nanostructured lipid carrier for brain targeting.Int. J. Pharm.20165061-2465610.1016/j.ijpharm.2016.04.033 27094357
    [Google Scholar]
  52. LiuJ.R. ChenG.F. ShihH.N. KuoP.C. Enhanced antioxidant bioactivity of Salvia miltiorrhiza (Danshen) products prepared using nanotechnology.Phytomedicine2008151-2233010.1016/j.phymed.2007.11.012 18077145
    [Google Scholar]
  53. Rahmati, Shima; Karimi, Hafez; Alizadeh, Morteza; Khazaei, Amir Hossein; Paiva-Santos, Ana Cláudia; Rezakhani, Leila Prospects of plant-derived exosome-like nanocarriers in oncology and tissue engineering.Hum. Cell202437112113810.1007/s13577‑023‑00994‑4
    [Google Scholar]
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