Difficulty Swallowing / Dysphagia Support
SprayNasalNon sterile Rx only

Naltrexone Nasal Spray (MucoLox™)

Mucoadhesive Nasal Base

A compounded naltrexone nasal spray in MucoLox, prepared in Chino, CA to a prescriber's order as an alternative route for low dose naltrexone therapy.

Reviewed by Linda Pungpravat, Compounding Pharmacist, RPh Mixwell Compounding Pharmacy, Chino, CA

  • USP <795> compliant
  • USP <800> hazardous drug lab
  • PCCA member

Clinical Advantages

  • Custom strength available
  • Alternative to swallowing pills
  • Measured dose applicator
  • Non sterile preparation

How It Works

What is Naltrexone Nasal Spray?

Naltrexone Nasal Spray is a compounded preparation of naltrexone, an opioid receptor antagonist, in MucoLox, a mucoadhesive nasal vehicle. It is prepared by prescription as a nasal route for low dose naltrexone therapy, most often for patients who cannot or prefer not to take an oral capsule.

How it works

  1. At the doses used in low dose naltrexone therapy, naltrexone is proposed to briefly block opioid receptors and modulate immune signaling, though the exact mechanism is not fully established [1].
  2. MucoLox is designed to hold the drug against the nasal mucosa longer than a plain liquid would, which may support absorption.
  3. Nasal delivery avoids first pass metabolism in the liver, which affects a drug taken by mouth.
  4. Published nasal naltrexone research does not test this low dose, chronic use case: one human study used a permeation enhancer and full opioid blocking doses for a single administration [2], and low dose intranasal naltrexone has been tested only in rodents given opioids at the same time [3].

When prescribers choose it

  • Prescribers whose patients cannot swallow or tolerate an oral capsule
  • Prescribers whose patients have gastrointestinal side effects with oral naltrexone
  • Prescribers already using low dose naltrexone who want a different route for a specific patient
  • Practices wanting a measured, low volume dose

Clinical Details

What does the evidence show?
  • Younger and colleagues (2013, Arthritis & Rheumatism) found that low dose oral naltrexone reduced pain in a small crossover trial of women with fibromyalgia [4]. This trial studied the oral capsule, not a nasal spray.
  • Due Bruun and colleagues (2024, The Lancet Rheumatology) randomized 99 women with fibromyalgia to oral naltrexone 6 mg daily or placebo and found no significant difference in pain, with a possible signal for memory problems [5]. An accompanying commentary described the result as another disappointment for the field [6].
  • Krieter and colleagues (2019, Journal of Clinical Pharmacology) gave healthy volunteers a single intranasal dose of naltrexone with a permeation enhancer and measured its pharmacokinetics against an intramuscular injection, in the context of a possible opioid overdose treatment. This was a pharmacokinetic study, not a trial of low dose naltrexone or of chronic pain [2].
  • Micheli and colleagues (2020, Frontiers in Pharmacology) gave mice and rats a low dose of intranasal naltrexone before morphine or oxycodone, and it reduced some gastrointestinal and cognitive side effects of the opioids without blocking pain relief. This was an animal study of naltrexone given alongside an opioid, not a study of naltrexone used on its own for a chronic condition, and no human study of low dose intranasal naltrexone has been published [3].

Findings come from the cited studies and do not promise any individual outcome.

Why is it compounded, and how is it typically used?

Why it is compounded

No FDA approved naltrexone product exists in a low dose strength, and no naltrexone nasal spray is commercially available in any strength [7]. A prescriber who wants naltrexone delivered nasally, rather than as the oral capsule most commonly used for low dose therapy, orders it compounded.

Dosage forms and strengths

  • Strength set by the prescriber, since no published low dose nasal regimen exists
  • MucoLox nasal vehicle
  • A metered spray pump for a consistent volume per dose
  • Dye free versions on request

There is no published dosing schedule for intranasal low dose naltrexone. Strength, frequency, and duration are the prescriber's decision, made without the trial evidence that supports the oral capsule.

How Mixwell prepares it

Mixwell compounds this spray in Chino, California under USP 795 standards for non sterile preparations [8]. Our pharmacist confirms the strength and the metered dose with the prescriber before compounding, and the label carries storage instructions. Batch records document every preparation, and finished sprays ship across California.

Safety information

Naltrexone's oral labeling no longer carries a boxed warning for liver injury; that warning was removed in 2013. Labeling still describes hepatocellular injury at doses well above those used for alcohol or opioid dependence, with the margin between an apparently safe dose and a harmful one estimated at fivefold or less, and low dose naltrexone therapy uses doses far below even the standard 50 mg dose [7].

Since no nasal formulation has been studied in people, how much naltrexone reaches the bloodstream by this route, and how consistently, is not established. Nasal irritation is possible with any nasal spray. Patients taking opioid pain medicines should not use naltrexone without their prescriber's direction, since it can precipitate withdrawal. Patient selection, dosing, monitoring, and duration are the prescriber's responsibility.

References
  1. Younger J, Parkitny L, McLain D. The use of low dose naltrexone as a novel anti inflammatory treatment for chronic pain. Clin Rheumatol. 2014;33(4):451 to 459. doi:10.1007/s10067-014-2517-2
  2. Krieter PA, Chiang N, Gyaw S, Skolnick P, Snyder R. Enhanced intranasal absorption of naltrexone by dodecyl maltopyranoside: implications for the treatment of opioid overdose. J Clin Pharmacol. 2019;59(9):1187 to 1195. doi:10.1002/jcph.1384
  3. Micheli L, Di Cesare Mannelli L, Lucarini E, et al. Intranasal low dose naltrexone against opioid side effects: a preclinical study. Front Pharmacol. 2020;11:576624. doi:10.3389/fphar.2020.576624
  4. Younger J, Noor N, McCue R, Mackey S. Low dose naltrexone for the treatment of fibromyalgia: findings of a small, randomized, double blind, placebo controlled, counterbalanced, crossover trial assessing daily pain levels. Arthritis Rheum. 2013;65(2):529 to 538.
  5. Due Bruun K, Christensen R, Amris K, et al. Naltrexone 6 mg once daily versus placebo in women with fibromyalgia: a randomised, double blind, placebo controlled trial. Lancet Rheumatol. 2024;6(1):e31 to e39. doi:10.1016/S2665-9913(23)00278-3
  6. Hauser W, Fitzcharles MA. Is low dose naltrexone for fibromyalgia another treatment disappointment? Lancet Rheumatol. 2024;6(1):e5 to e6. doi:10.1016/S2665-9913(23)00297-7
  7. Naltrexone hydrochloride tablets, 50 mg. Prescribing information. DrugCentral label
  8. United States Pharmacopeia. General Chapter 795, Pharmaceutical Compounding: Nonsterile Preparations. USP NF. Official November 1, 2023.

What to include on the prescription

  • APIs and strengths
  • Base or vehicle
  • Quantity
  • Directions for use
  • Refills
  • Allergies or dye free needs
Call (909) 378-7301 Fax (909) 378-7071

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Compounded in Chino, CA. Delivered across California.

  • Chino
  • Chino Hills
  • Ontario
  • Pomona
  • Diamond Bar
  • Rancho Cucamonga
  • Eastvale
Mixwell Compounding Pharmacy 13788 Roswell Ave, Ste 158, Chino, CA 91710
(909) 378-7301

Compounded medications are not reviewed or approved by the FDA. Dispensed only with a valid prescription. Mixwell is a non sterile pharmacy and does not prepare sterile products or injectables. Compounded preparations are not presented as superior to commercially available products, and nothing here promises a specific result. Mixwell does not accept insurance. Call for pricing.

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Want to learn more about Naltrexone Nasal Spray (MucoLox™)

Are you a healthcare provider or patient in Chino, Chino Hills, Ontario, Eastvale, Rancho Cucamonga, or Upland? Mixwell Pharmacy provides specialized pharmaceutical support throughout San Bernardino, Los Angeles, and Orange Counties. Contact our Chino laboratory to learn how we facilitate customized Naltrexone Nasal Spray (MucoLox™)for practitioners across Southern California.

(909) 378-7301

Serving Los Angeles County, Orange County, San Bernardino County, Riverside County, Ventura County, and the Inland Empire