NADIFLOXACIN AND ADAPALENE: A REVIEW ON REPORTED METHODS FOR PURPOSE OF VALIDATION AND QUALITY MONITORING

NADIFLOXACIN AND ADAPALENE: A REVIEW ON REPORTED METHODS FOR PURPOSE OF VALIDATION AND QUALITY MONITORING

S. N. Naik * and Z. R. Dedania

Department of Pharmaceutical Quality Assurance, Rofel Shri G. M. Bilakhia College of Pharmacy, Vapi, Gujarat, India.

ABSTRACT: Acne vulgaris is a common chronic inflammatory skin disease found predominantly in adolescents in both sexes. The best acne treatment inhibits bacterial growth, encourages the shedding to the skin cells to unclog pores. Treatment for acne includes topical agents and systemic agents. Its quality monitoring becomes essential for assuring quality products for human care. So, for that purpose a detailed study of review was done including reported and validated methods, official monograph methods for estimation of Nadifloxacin and Adapalene. It was found from a literature survey that among all reported evaluation methods the most widely and predominantly followed method is HPLC. Other methods reported were UV, HPTLC. A conclusion was made that there is lack of evaluation analytical methods for simultaneous estimation of Nadifloxacin and Adapalene in combined dosage form.

Keywords: Nadifloxacin, Adapalene, Chromatography, Column, Mobile phase

INTRODUCTION: Acne vulgaris is common chronic inflammatory skin disease found predominantly in adolescents in both sexes. The lesion is formed which are more commonly seen on the face, on upper chest and upper back. The appearance of lesions near puberty is due to physiological hormonal variation. Mild acne is defined as presence of clogged skin follicles which is also known as comedones on to the face with inflammatory lesions. People with mild acne don’t get large areas of red, inflamed skin or acne scarring.

Moderate acne occurs when a high number of inflammatory papules and pustules occur on the face when compared to mild cases of acne. They are also found on the trunk of the body. Severe acne occurs when nodules (which is also called as painful bumps) are the characteristic facial lesions and the involvement of trunk is more. Sign and symptoms of acne varies depending upon severity of condition: White heads, Black heads, Small red tender bumps, Pimples, painful lumps (nodules).

Androgen stimulates secretion of the sebaceous gland causing them to enlarge and secrete the natural oil, sebum which rises up to top of the hair follicle and flows out on to the skin surface. In adults who develop acne, androgenic stimulation produces a high response in the sebaceous gland so, the formation of acne occurs when accumulated sebum plugs the pilosebaceous ducts.

This accumulated material leads to the formation of comedones. Treatment: The best acne treatment inhibits bacterial growth, encourages the shedding to the skin cells to unclog pores. Treatment for acne includes topical agents and systemic agents. Topical agents used in treatment of acne vulgaris: Treatment of acne vulgaris involves retinoids and antimicrobial and some antibacterial drug use. Topical retinoid acts to normalise the maturation of follicular epithelium and reduces inflammation and enhances the penetration of topical medication.

Nadifloxacin is a topical antibiotic that treats bacterial skin infections and acne. It's a second-generation fluoroquinolone that's effective against aerobic and anaerobic bacteria, including Gram-negative bacteria, Gram-positive bacteria, Propionibacterium species, Streptococcus species, and Staphylococcus species. Nadifloxacin works by preventing the synthesis of essential proteins and inhibiting the activity of bacterial enzymes. Nadifloxacin is intended for external use only. Some side effects that may occur during treatment include burning and itching, contact dermatitis, dryness, and skin irritation ¹.

Adapalene is a third generation topical retinoid primarily used in the treatment of mild-moderate acne, and is also used off-label to treat keratosis pilaris as well as other skin conditions. Studies have found adapalene is as effective as other retinoids, while causing less irritation. It also has several advantages over other retinoids ². The adapalene molecule is more stable compared to tretinoin and tazarotene, which leads to less concern for photodegradation.

Nadifloxacin ^{3, 4}:

FIG. 1: STRUCTURE OF NADIFLOXACIN

It is also chemically more stable compared to the other two retinoids, allowing it to be used in combination with benzoyl peroxide. Due to its effects on keratinocyte proliferation and differentiation, adapalene is superior to tretinoin for the treatment of comedonal acne and is often used as a first-line agent.

Chemical Name: 9-Fluoro – 8 - (4 – hydroxyl - 1-piperidinyl) – 5 – methyl – 1 – oxo - 6, 7-dihydro-1H, 5Hpyrido[3, 2,1-ij] quinoline-2-carboxylic acid

Molecular Formula: C₁₉H₂₁FN₂O₄

Molecular weight 360.379 g/mol

Drug Category: Antibacterial

Mechanism of action: Inhibits enzyme DNA gyrase that is involved in bacterial DNA synthesis and replication, thus inhibiting the bacterial multiplication.

Indication: Used in treatment of bacterial skin infection i.e. acne vulgaris

Adapalene ^{5, 6, 7}:

FIG. 2: STRUCTURE OF ADAPALENE

Chemical Name: 6 - [3 - (adamantan – 1 - yl) - 4- methoxyphenyl] naphthalene -2-carboxylic acid.

Molecular Formula: C₂₈H₂₈O₃

Molecular Weight: 412.52 g/mol

Drug Category: Topical retinoid

Mechanism of Action: It acts on retinoid receptor. It is modulator of cell differentiation, keratinization and inflammatory processes which is pathology of acne vulgaris. Indication Used in treatment of acne vulgaris.

Mechanism of Action (in Combination): Nadifloxacin is an antibiotic. It kills bacteria by preventing them from reproducing and repairing themselves.

Adapalene is a form of vitamin A which prevents accumulation of sebum (skin's natural oil), unblocks the pores and allows natural exfoliation of the outer layers of skin. Combination is approved by CDSCO on 17-7-2015. The gel is used in acne vulgaris. The dose is 10 mg of nadifloxacin and 1mg of adapalene.

FIG 3: COMBINATION MARKETED FORMULATION

Method for Analysis: Quality monitoring is essential to certify the quality, safety, and efficacy of pharmaceutical products. So, Analytical Methods are developed and validated as per ICH guideline to assure quality. The methods reported in the literature for evaluation of Nadifloxacin and Adapalene were UV-Visible spectroscopy, HPLC, HPTLC, UPLC. The summary of reported methods is shown in Fig. 4 and Fig. 5.

Literature review shows that many methods has been developed for Nadifloxacin but with other drugs like Mometasone furoate, Terbinafine hydrochloride, Clobetasol Propionate and Miconazole nitrate and also for adapalene in combination with other drugs like Benzoyl peroxide, Clindamycin Phosphate. But no method has been reported for simultaneous estimation of Nadifloxacin and Adapalene. The summary of reported methods is depicted in below Table 1 and Table 2.

FIG. 4: REPORTED METHODS OF NADIFLOXACIN FROM LITERATURE SURVEY            

FIG. 5: REPORTED METHODS OF ADAPALENE FROM LITERATURE SURVEY

TABLE 1: REPORTED METHODS FOR NADIFLOXACIN

TABLE 2: REPORTED METHODS FOR ADAPALENE

CONCLUSION: This review shows detailed study on the reported Spectroscopic and Chromato-graphic methods developed and validated for the estimation of Nadifloxacin and Adapalene. Literature review suggest that there are various spectroscopic and chromatographic methods available for the estimation of Nadifloxacin and Adapalene alone and in combination with other drugs. HPLC and HPTLC methods were found to be very common.

There is only one HPLC reported method for Nadifloxacin and Adapalene in their combined dosage form. So, there will be a great scope for the method development and validation of same with good precision, accuracy and robust methods for available marketed combined dosage form of Nadifloxacin and Adapalene.

ACKNOWLEDGEMENT: Nil

CONFLICTS OF INTEREST: Nil

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    How to cite this article:

    Naik SN and Dedania ZR: Nadifloxacin and adapalene: a review on reported methods for purpose of validation and quality monitoring. Int J Pharm Sci & Res 2025; 16(3): 655-62. doi: 10.13040/IJPSR.0975-8232.16(3).655-62.

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