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Table 1 Experimental studies with local anesthetics encapsulated into various nanoparticles

From: Recent advances in pain management based on nanoparticle technologies

Local anesthetic drug

Nanoparticles

Subjects (administration route)

Antinociceptive test

Results

Ref

Benzocaine

PLGA, PLA, PCL

Mice (injection into the popliteal space)

PWTP

Pharmacological assessment indicated that encapsulation of benzocaine in polymeric nanocapsules prolonged its anesthetic effect compared with free benzocaine

[83]

Lidocaine/prilocaine

Polymeric nanocapsules

Rat (oral mucosa)

Tail-flick

The formulation provided effective and longer-lasting superficial anesthesia at the intraoral mucosa during medical and dental procedures

[84]

Bupivacaine

Alginate/chitosan (ALG–CHIT)-Alginate/bis (2-ethylhexyl) sulfosuccinate (ALG–AOT)

Mice (popliteal space)

PWTP

Comparison among formulations displayed that 0.125% bupivacaine-loaded ALG–CHIT and bupivacaine-loaded ALG–AOT improved the analgesia 1.5- and 2.16-fold, respectively, compared with plain bupivacaine

[85]

Ropivacaine

Liposome

Human (oral mucosa)

Pinprick test

Extensive soft tissue anesthesia was achieved using liposome containing ropivacaine and EMLA group, when compared with ropivacaine and benzocaine gels (P < 0.0001)

[86]

Tetracaine

Liposome

Human (skin)

McNemars test

The formulation produced better superficial local anesthesia than EMLA

[87]

Bupivacaine

Alginate/chitosan

Rabbit-rat (intraoral or intrathecal injections)

Observation of the aversive response to the rat upper lip pinching

The analgesic properties of bupivacaine increased 1.4-fold (P < 0.001) with bupivacaine 0.5%-loaded alginate–chitosan nanoparticles after infraorbital nerve blockade

[88]

Tetrodotoxin

Hollow silica nanoparticles

Rat (sciatic nerve injection)

Neuro-behavioral testing

The sustained release of tetrodotoxin encapsulated in hollow silica nanoparticles with diameter of 28 nm prolonged duration of action and at the same time reduced systemic toxicity

[89]

Tetrodotoxin

Poly(triol dicarboxylic acid)-co-poly(ethylene glycol)

Rat (sciatic nerve injection)

Neuro-behavioral testing

Tetrodotoxin released from polymers created nerve block duration, from several hours to 3 days, with insignificant local or systemic toxicity

[90]

  1. PWTP paw withdrawal threshold to pressure, PLGA poly(lactic-co-glycolic acid), PLA polylactic acid, PCL polycaprolactone, EMLA eutectic mixture of local anesthetics