# Single-administration microneedles with controlled sustained release of non-opioid analgesics to treat osteoarthritis pain

> **NIH NIH R21** · UNIVERSITY OF CONNECTICUT STORRS · 2023 · $214,062

## Abstract

Abstract
Every year, millions of people suffer from arthritis such as osteoarthritis, a disease associated with extreme joint
pain and inflammation. Despite the strong effect of opioids for pain treatment, the drug causes serious problems
of drug abuse and addiction. Alternatively, other analgesics including NSAIDs (non-opiate and non-steroid anti-
inflammation drugs) and glucocorticoids have been traditionally prescribed to alleviate OA pain without the
concern of opioid addiction. These drugs also have limitations, which are largely due to the routes of
administration. Oral tables struggle with the first-pass metabolism, thus requiring a large amount of drugs and
easily leading to severe systemic side effects. For example, NSAID drugs often have low bioavailability and are
prescribed with a large oral dose of 300-1000 mg/day, which causes significant GI problems (e.g. stomach
bleeding, and stomach ulcers), retinal disfunction, cardiovascular diseases etc. Glucocorticoid tablets, when
used with a large quantity, also exhibit side effects of lower resistance to infection, higher risk of osteoporosis
etc.12. Besides oral delivery, intra-articular (IA) injections of pain medicines, especially for glucocorticoids such
as Dexamethasone (Dex)13, 14, have shown the efficacy to treat OA pain. However, the injections need to be
repeated multiple times to sustain the analgesic effect, posing significant problems of complexity, cost, and
inconvenience, leading to low patient compliance/adherence. The invasiveness of repeated IA injections could
also cause more cartilage damages. In this regard, transdermal microneedles (MNs) have appeared as a
powerful system to penetrate the SC, facilitating the intra-skin delivery of various drugs. Tiny MNs avoid touching
the nerve endings to tremendously reduce pain and can be even self-administered by non-professionals,
significantly increasing patient compliance. Here, we propose a novel (trans)dermal biodegradable MN
system which can be fully embedded into the skin at a single-time to perform a well-controlled sustained
release of non-opioid analgesics over a long period for the treatment of chronic musculoskeletal pains.
Our objective in this R21 is to develop a single-time skin administration MN patch to perform a long-term delivery
of a common non-opioid glucocorticoid, Dexamethasone or Dex (as a drug model). These MNs will be the first
transdermal system to provide a separate control over the release dose and the release period, which can
be easily extended over a long period to treat chronic OA pain. Our overarching hypothesis is that patients
with OA/arthritis pains would be able to self-apply such a MN patch on the skin even at home (similar to a wound
bandage) at just a single time to obtain a long-term pain relief, similar to the analgesic effect obtained from the
repeated IA injections. We design our project with two specific aims; Aim 1 is to characterize the release kinetics
of the core-shell MNs and engi...

## Key facts

- **NIH application ID:** 10618335
- **Project number:** 5R21AR080919-02
- **Recipient organization:** UNIVERSITY OF CONNECTICUT STORRS
- **Principal Investigator:** Thanh Nguyen
- **Activity code:** R21 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2023
- **Award amount:** $214,062
- **Award type:** 5
- **Project period:** 2022-05-05 → 2026-04-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10618335

## Citation

> US National Institutes of Health, RePORTER application 10618335, Single-administration microneedles with controlled sustained release of non-opioid analgesics to treat osteoarthritis pain (5R21AR080919-02). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10618335. Licensed CC0.

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