Abstract
Objective: The objective of this study is to optimize a nanosponge formulation for Loxoprofen and then incorporating it into a gel formulation offering a controlled drug release, enhanced skin permeation and thus better bioavailability. Methods: Loxoprofen nanosponges were prepared using the emulsion solvent diffusion method and formulated using Polyvinyl alcohol, Ethylcellulose and Dichloromethane. The effect of the different formulation variables like ethyl cellulose: polyvinyl alcohol ratio, drug: ethyl cellulose ratio, stirring time, stirring speed, internal phase volume and external phase volume on the particle size, entrapment efficiency, production yield, polydispersity index and Zeta potential was investigated. The optimized nanosponge formulation was incorporated into a gel. The loaded gel was evaluated by in vitro release and permeation studies and the results were compared to that of a marketed formulation (Loxonin® gel). Results: The optimized formulation showed 67.29±1.19 % entrapment efficiency, 239.8±16.95 nm particle size and-8.32±0.87 mV Zeta potential. The drug was released slowly from the nanosponge-loaded gel where the cumulative percentage of drug released was only 77.71±0.42 % in 8 h where it was incorporated in the entrapped form while it was 99.31±0.64% from Loxonin® gel where it was in the unentrapped form. The cumulative percent of drug permeated through the skin from the nanosponge-loaded gel was 98.66±0.14% for 24 h while it was only 60.38±0.18% from Loxonin® gel. Conclusion: The nanosponge-loaded gel showed more sustained drug release and a better drug permeation when compared to a marketed gel (Loxonin® gel).
Highlights
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most frequently prescribed drug groups. These drugs are used locally or systemically in the treatment of various chronic inflammatory conditions, relieving pain, reducing fever, and preventing local inflammation [2], NSAIDs lead to unfavorable effects on the stomach as a result of inhibition of prostaglandins, which play a role in the protection of the gastric mucosa
In order to assess the effect of ethyl cellulose (EC): polyvinyl alcohol (PVA) ratio on the physicochemical characteristics of nanosponges, six formulations with different EC: PVA ratios were prepared
This may be due to the increased foaming during the nanosponge preparation with the increase in the amount of PVA hindering the formation of the nanosponges [29]
Summary
Osteoarthritis is a leading cause of disability among older adults worldwide. Treatment aims are to alleviate inflammatory pain and improve physical function through non-pharmacological and pharmacological interventions. NSAIDs are among the most frequently prescribed drug groups These drugs are used locally or systemically in the treatment of various chronic inflammatory conditions, relieving pain, reducing fever, and preventing local inflammation [2], NSAIDs lead to unfavorable effects on the stomach as a result of inhibition of prostaglandins, which play a role in the protection of the gastric mucosa. Conventional transdermal delivery systems such as ointments and creams are associated with side effects due to the uncontrolled drug release from the formulation. A wide variety of topical agents can be safely incorporated into nanosponges for getting the benefits of these systems [7] They are non-irritating, non-mutagenic, nonallergenic, non-toxic [8] and can serve as a local depot for sustained drug release, facilitate drug permeation across the skin, improve the bioavailability, increase the stability, reduce drug toxicity and irritation, decrease adverse effects and improve the patient compliance by prolonging the dosage intervals [9], and overcoming the limitations of conventional transdermal delivery systems. The objective of the present study is to assess the applicability of formulating nanosponges of Loxoprofen sodium and incorporating them into a transdermal gel and comparing this nanosponge-loaded gel to conventional gels to clarify the advantages of the nanosponges technology
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