Nefopam hydrochloride loaded microspheres for post-operative pain management: synthesis, physicochemical characterization and in-vivo evaluation.
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 <5% which signified haemocompatibility of formulation. ED50 in rat tail-flick anti-nociceptive test was found ∼18.12 mg/kg. In post-operative pain model, reversal of mechanical allodynia and thermal hyperalgesia by NPH-MS was statistically significant (p < .001) as compared with NPH till 24 h post-dose.
a Chitkara College of Pharmacy, Chandigarh-Patiala National Highway , Rajpura, Patiala , Punjab , India.|b Department of Research, Innovation and Consultancy , IKG Punjab Technical University , Jalandhar-Kapurthala Highway , Kapurthala , Punjab , India.
Neelam
N
Sharma
a Chitkara College of Pharmacy, Chandigarh-Patiala National Highway , Rajpura, Patiala , Punjab , India.
Sandeep
S
Arora
c Chandigarh College of Pharmacy, Landran , Kharar , Punjab , India.
Jitender
J
Madan
D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D055598:Chemical Phenomena; D060326:Chemistry Techniques, Synthetic; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D006885:Hydroxybutyrates / Q000737:chemistry; D006930:Hyperalgesia / Q000188:drug therapy; D008422:Materials Testing; D008863:Microspheres; D009340:Nefopam / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D010149:Postoperative Pain / Q000188:drug therapy*; D011091:Polyesters / Q000737:chemistry; D051381:Rats; D000094122:Polyhydroxybutyrates
D000700:Analgesics; D004337:Drug Carriers; D006885:Hydroxybutyrates; D009340:Nefopam; D011091:Polyesters; C016240:polycaprolactone; C003182:poly-beta-hydroxybutyrate; D000094122:Polyhydroxybutyrates
Poly-3-hydroxybutyrate; anti-nociceptive; haemocompatibility; mechanical allodynia; poly-(ɛ-caprolactone); post-operative pain model; sustained release microspheres; thermal hyperalgesia