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Application of computational tools for the designing of Oleuropein loaded nanostructured lipid carrier for brain targeting through nasal route

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Abstract

Purpose

Meningitis is an inflammation of meninges encircled the brain and spinal cord. Currently it can be treated with second generation cephalosporins which were ended up with an unresolvable problem called Multi Drug Resistance (MDR). Hence, there is a need to develop a better herbal molecule to conflict the MDR.

Methods

Hot Blanching technique followed by ultra sound assisted extraction using bio-solvent aqueous glycerol was used to extract OLE from olive leaves. QbD tool was applied to predict the interactions between Critical Material Attributes (Ratio of solid Lipid X1, Concentration of Surfactant X2) and Critical Process Parameters (Homogenization Time X3) on Critical Quality Attributes (CQA, Particle Size Y1, Zeta Potential Y2, and Entrapment Efficiency Y3). Particulate characteristics were evaluated and Invivo pharmacokinetic study was done in albino Wistar rats by IV and IN route of administration.

Results

Thermal studies reflect the formation of low ordered crystalline structure of lipid matrix which offers higher encapsulation of drug in NLC than physical mixture. CMA and CPP show significant effect on CQA and method operable design range was developed. Histo-pathological studies confirms that there is no signs of toxicity and in-vitro drug release studies reveals a rapid release of a drug initially followed by prolonged release of oleuropein upto 24 h. The absolute bioavailability of drug loaded NLC in brain was higher in IN route compared to NLC administered by IV route.

Conclusions

In a nutshell, challenges offered by the hydrophilic OLE for brain targeting can be minimized through lipidic nature of NLC.

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Acknowledgements

The Principal Author acknowledges financial support from Department of Science and Technology (DST-Women Scientist Scheme) for this project (DST Ref No: SR/WOS-A/LS-1262/2015(G) Dated 30.05.2016). Authors also highly thankful to Dr.R.Venkataswamy, Chairman and Mr. R.V. Srinivas, Vice-Chairman, Sri Venkateswara College of Pharmacy, RVS Nagar, Chittoor, Andhra Pradesh to pursue and successful competition of this research work.

Funding

The principal author acknowledges the financial support from Department of Science andTechnology (DST) – Women Scientist Scheme (WOS-A) for this project (DST No: SR/WOS-A/LS-1262- 2015 dated 30.05.2016).

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Authors and Affiliations

  1. Department of Pharmaceutics, Jawaharlal Nehru Technological University Anantapur, Ananthapuramu, Andhra Pradesh, 515001, India

    Sucharitha Palagati

  2. Department of Pharmaceutics, Sri Venkateswara College of Pharmacy, RVS Nagar, Chittoor, Andhra Pradesh, 517127, India

    Sucharitha Palagati

  3. Department of Chemical Engineering, Jawaharlal Nehru Technological University Anantapur, Ananthapuramu, Andhra Pradesh, 515001, India

    Satyanarayana SV

  4. Department of Pharmaceutics, Centre for Nanotechnology, Sri Venkateswara College of Pharmacy, Chittoor, Andhra Pradesh, 517127, India

    Bhaskar Reddy Kesavan

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Correspondence to Sucharitha Palagati.

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Palagati, S., SV, S. & Kesavan, B.R. Application of computational tools for the designing of Oleuropein loaded nanostructured lipid carrier for brain targeting through nasal route. DARU J Pharm Sci 27, 695–708 (2019). https://doi.org/10.1007/s40199-019-00304-0

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