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  • 15/03/20, 11)54 PMNefopam hydrochloride loaded microspheres for post-operative pain… Artificial Cells, Nanomedicine, and Biotechnology: Vol 46, No 1

    Page 1 of 19https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459

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    Volume 46, 2018 - Issue 1

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    Original Articles

    Nefopam hydrochloride loaded

    microspheres for post-operative pain

    management: synthesis,

    physicochemical characterization

    and in-vivoin-vivo evaluation ,Neelam Sharma # &Sandeep Arora Jitender Madan

    Pages 138-146 | Received 22 Nov 2016, Accepted 27 Feb 2017, Published online: 21 Mar 2017

    $ Download citation % https://doi.org/10.1080/21691401.2017.1301459

    &&In this article

    Abstract

    Graphical Abstract

    Introduction

    Materials and methods

    Results and discussion

    Conclusions

    References

    Abstract

    Once-daily oral dosage of nefopam hydrochloride loaded

    sustained release microspheres (NPH-MS) was investigated as

    novel therapeutic strategy for post-operative pain management.

    Microspheres were synthesized using poly-3-hydroxybutyrate and

    poly-(ɛ-caprolactone) by double emulsion solvent evaporation

    technique. NPH-MS were characterized through FTIR, PXRD and

    SEM. In-vitro drug release study revealed sustained behavior till

    24 h. Haemolysis was

  • 15/03/20, 11)54 PMNefopam hydrochloride loaded microspheres for post-operative pain… Artificial Cells, Nanomedicine, and Biotechnology: Vol 46, No 1

    Page 2 of 19https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459

    Keywords: Poly-3-hydroxybutyrate, poly-(ɛ-caprolactone), sustained release

    microspheres, haemocompatibility, anti-nociceptive, mechanical

    allodynia, thermal hyperalgesia, post-operative pain model

    Introduction

    The investigations in drug delivery involve sustained release of an

    active entity to curtail dosage frequency, diminution in toxicity

    though retaining therapeutic effectiveness of dosage regimen,

    improved bioavailability of active pharmaceutical moiety with

    superior safety and biocompatibility [1]. Nefopam hydrochloride

    (NPH) (Figure 1(a)) is non-opioid centrally acting analgesic

    preferred for relief of nociception in different pain syndrome such

    as acute traumatic, surgical operations, toothache and myalgia.

    Recommended oral dosage of NPH is 30–90 mg three times daily

    which might produce patient non-compliance and additional side

    effects such as dry mouth, hypersensitivity, patch necrosis of

    gastrointestinal mucosa, nausea and vomiting [2,3]. Therefore,

    development of biodegradable sustained release polymeric

    microspheres of NPH has been superlative methodology to

    reduce dosage frequency [4].

    Figure 1. Chemical structure of (a) nefopam hydrochloride, (b)

    poly-3-hydroxybutyrate, and (c) poly-ɛ-caprolactone.

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    https://www.tandfonline.com/keyword/Poly-3-hydroxybutyrate https://www.tandfonline.com/keyword/Poly-%28%C9%9B-caprolactone%29 https://www.tandfonline.com/keyword/Sustained+Release+Microspheres https://www.tandfonline.com/keyword/Haemocompatibility https://www.tandfonline.com/keyword/Anti-nociceptive https://www.tandfonline.com/keyword/Mechanical+Allodynia https://www.tandfonline.com/keyword/Thermal+Hyperalgesia https://www.tandfonline.com/keyword/Post-operative+Pain+Model https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459# https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459# https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459# https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459# https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459# https://www.trendmd.com/how-it-works-readers https://iopscience.iop.org/article/10.1088/1674-1056/27/11/117701?utm_source=trendmd&utm_campaign=china&utm_medium=cpc https://www.sciencedirect.com/science/article/pii/S025296021830849X?utm_source=TrendMD&utm_medium=cpc&utm_campaign=Acta_Mathematica_Scientia_TrendMD_1 https://link.springer.com/article/10.1007/s40820-018-0234-0?utm_source=TrendMD&utm_medium=cpc&utm_campaign=Nano-Micro_Letters_TrendMD_1 https://www.sciencedirect.com/science/article/pii/S2095268618301083?utm_source=TrendMD&utm_medium=cpc&utm_campaign=International_Journal_of_Mining_Science_and_Technology_TrendMD_1 https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1304406?src=recsys https://www.tandfonline.com/author/Dabbaghi%2C+Maryam

  • 15/03/20, 11)54 PMNefopam hydrochloride loaded microspheres for post-operative pain… Artificial Cells, Nanomedicine, and Biotechnology: Vol 46, No 1

    Page 3 of 19https://www.tandfonline.com/doi/full/10.1080/21691401.2017.1301459

    Poly-3-hydroxybutyrate (PHB) (Figure 1(b)) and poly-ɛ-

    caprolactone (PCL) (Figure 1(c)) had been utilized as drug carriers

    owing to their biodegradability via hydrolytic cleavage of ester

    bonds into non-toxic end-products which can be eliminated from

    body via natural metabolic pathways [5–7]. Since, amorphous

    regions of semicrystalline PCL degrade prior to crystalline

    domains leading to change in drug release profile. Therefore,

    blend of PHB and PCL merge specific characteristic from

    individual polymer for controlling drug release pattern from

    microspheres [8–10].

    In current investigation, novel sustained release nefopam

    hydrochloride loaded microspheres (NPH-MS) were

    manufactured for effective management of post-operative pain

    condition. Antinociceptive tail-flick activity of NPH-MS was

    executed to determine its effective oral dose (ED ) in rat model.

    Magnitude of reversal of mechanical allodynia and thermal

    hyperalgesia produced by NPH-MS was compared with NPH using

    post-operative pain model. Behavioral signs of allodynia and

    hyperalgesia were von frey withdrawal threshold (VFWT) and paw

    withdrawal latency (PWL) in von Frey and plantar test,

    respectively.

    Materials and methods

    Materials

    Poly ɛ-caprolactone (CAS No-24980-41-4, (C H O ) , average M

    ∼14,000, average M ∼10,000 by GPC) and polyhydroxybutyrate

    (CAS No-29435-48-1, poly-(R)-3-hydroxybutyric acid) were

    purchased from Sigma–Aldrich Chemie, Gmbh, Steinhelm,

    Germany. Nefopam hydrochloride (M 289.8 g/mol, 99.57%

    purity) was purchased from Hangzhou-Daying-Chem. Company

    Ltd., China. All other chemicals used were of analytical grade.

    Fabrication of NPH-loaded PHB/PCL biodegradable

    microspheres

    NPH-MS were fabricated using double emulsion solvent

    evaporation technique (Figure 2) [11,12]. Briefly, aqueous solution

    of NPH (1 part) was prepared in distilled water:acetone (1:1)

    mixture. Polymer blend (3 part) containing PHB:PCL (1:1) was

    incorporated in dichloromethane (10 mL) to produce organic

    50

    6 10 2 n w

    n

    w

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  • 15/03/20, 11)54 PMNefopam hydrochloride loaded microspheres for post-operative pain… Artificial Cells, Nanomedicine, and Biotechnology: Vol 46, No 1