Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy
Oral candidiasis encompasses fungal infections of the tongue and other oral mucosal sites with fungal overgrowth and its invasion of superficial oral tissues. Borneol was assessed in this research as the matrix-forming agent of clotrimazole-loaded in situ forming gel (ISG) comprising clove oil as th...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-05-01
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| Series: | Gels |
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| Online Access: | https://www.mdpi.com/2310-2861/9/5/412 |
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| author | Nutdanai Lertsuphotvanit Sarun Tuntarawongsa Kritamorn Jitrangsri Thawatchai Phaechamud |
| author_facet | Nutdanai Lertsuphotvanit Sarun Tuntarawongsa Kritamorn Jitrangsri Thawatchai Phaechamud |
| author_sort | Nutdanai Lertsuphotvanit |
| collection | DOAJ |
| description | Oral candidiasis encompasses fungal infections of the tongue and other oral mucosal sites with fungal overgrowth and its invasion of superficial oral tissues. Borneol was assessed in this research as the matrix-forming agent of clotrimazole-loaded in situ forming gel (ISG) comprising clove oil as the co-active agent and <i>N</i>-methyl pyrrolidone (NMP) as a solvent. Their physicochemical properties, including pH, density, viscosity, surface tension, contact angle, water tolerance, gel formation, and drug release/permeation, were determined. Their antimicrobial activities were tested using agar cup diffusion. The pH values of clotrimazole-loaded borneol-based ISGs were in the range of 5.59–6.61, which are close to the pH of 6.8 of saliva. Increasing the borneol content in the formulation slightly decreased the density, surface tension, water tolerance, and spray angle but increased the viscosity and gel formation. The borneol matrix formation from NMP removal promoted a significantly (<i>p</i> < 0.05) higher contact angle of the borneol-loaded ISGs on agarose gel and porcine buccal mucosa than those of all borneol-free solutions. Clotrimazole-loaded ISG containing 40% borneol demonstrated appropriate physicochemical properties and rapid gel formation at microscopic and macroscopic levels. In addition, it prolonged drug release with a maximum flux of 370 µg·cm<sup>−2</sup> at 2 days. The borneol matrix generated from this ISG obsentively controlled the drug penetration through the porcine buccal membrane. Most clotrimazole amounts still remained in formulation at the donor part and then the buccal membrane and receiving medium, repectively. Therefore, the borneol matrix extended the drug release and penetration through the buccal membrane efficiently. Some accumulated clotrimazole in tissue should exhibit its potential antifugal activity against microbes invading the host tissue. The other predominant drug release into the saliva of the oral cavity should influence the pathogen of oropharyngeal candidiasis. Clotrimazole-loaded ISG demonstrated efficacious inhibition of growth against <i>S. aureus</i>, <i>E. coli</i>, <i>C. albicans</i>, <i>C. krusei</i>, <i>C. Lusitaniae</i>, and <i>C. tropicalis</i>. Consequently, the clotrimazole-loaded ISG exhibited great potential as a drug delivery system for oropharyngeal candidiasis treatment by localized spraying. |
| first_indexed | 2024-03-11T03:43:01Z |
| format | Article |
| id | doaj.art-cdd6d161b39140d9aa24d6dd51f003bf |
| institution | Directory Open Access Journal |
| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-11T03:43:01Z |
| publishDate | 2023-05-01 |
| publisher | MDPI AG |
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| spelling | doaj.art-cdd6d161b39140d9aa24d6dd51f003bf2023-11-18T01:28:09ZengMDPI AGGels2310-28612023-05-019541210.3390/gels9050412Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis TherapyNutdanai Lertsuphotvanit0Sarun Tuntarawongsa1Kritamorn Jitrangsri2Thawatchai Phaechamud3Program of Pharmaceutical Technology, Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, ThailandPharmaceutical Intellectual Center “Prachote Plengwittaya”, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, ThailandDepartment of Chemical Engineering and Pharmaceutical Chemistry, School of Engineering and Technology, Walailak University, Nakhon Srithammarat 80160, ThailandProgram of Pharmaceutical Technology, Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, ThailandOral candidiasis encompasses fungal infections of the tongue and other oral mucosal sites with fungal overgrowth and its invasion of superficial oral tissues. Borneol was assessed in this research as the matrix-forming agent of clotrimazole-loaded in situ forming gel (ISG) comprising clove oil as the co-active agent and <i>N</i>-methyl pyrrolidone (NMP) as a solvent. Their physicochemical properties, including pH, density, viscosity, surface tension, contact angle, water tolerance, gel formation, and drug release/permeation, were determined. Their antimicrobial activities were tested using agar cup diffusion. The pH values of clotrimazole-loaded borneol-based ISGs were in the range of 5.59–6.61, which are close to the pH of 6.8 of saliva. Increasing the borneol content in the formulation slightly decreased the density, surface tension, water tolerance, and spray angle but increased the viscosity and gel formation. The borneol matrix formation from NMP removal promoted a significantly (<i>p</i> < 0.05) higher contact angle of the borneol-loaded ISGs on agarose gel and porcine buccal mucosa than those of all borneol-free solutions. Clotrimazole-loaded ISG containing 40% borneol demonstrated appropriate physicochemical properties and rapid gel formation at microscopic and macroscopic levels. In addition, it prolonged drug release with a maximum flux of 370 µg·cm<sup>−2</sup> at 2 days. The borneol matrix generated from this ISG obsentively controlled the drug penetration through the porcine buccal membrane. Most clotrimazole amounts still remained in formulation at the donor part and then the buccal membrane and receiving medium, repectively. Therefore, the borneol matrix extended the drug release and penetration through the buccal membrane efficiently. Some accumulated clotrimazole in tissue should exhibit its potential antifugal activity against microbes invading the host tissue. The other predominant drug release into the saliva of the oral cavity should influence the pathogen of oropharyngeal candidiasis. Clotrimazole-loaded ISG demonstrated efficacious inhibition of growth against <i>S. aureus</i>, <i>E. coli</i>, <i>C. albicans</i>, <i>C. krusei</i>, <i>C. Lusitaniae</i>, and <i>C. tropicalis</i>. Consequently, the clotrimazole-loaded ISG exhibited great potential as a drug delivery system for oropharyngeal candidiasis treatment by localized spraying.https://www.mdpi.com/2310-2861/9/5/412oropharyngeal candidiasisclotrimazoleborneolsolvent removalin situ forminggel |
| spellingShingle | Nutdanai Lertsuphotvanit Sarun Tuntarawongsa Kritamorn Jitrangsri Thawatchai Phaechamud Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy Gels oropharyngeal candidiasis clotrimazole borneol solvent removal in situ forming gel |
| title | Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy |
| title_full | Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy |
| title_fullStr | Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy |
| title_full_unstemmed | Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy |
| title_short | Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy |
| title_sort | clotrimazole loaded borneol based in situ forming gel as oral sprays for oropharyngeal candidiasis therapy |
| topic | oropharyngeal candidiasis clotrimazole borneol solvent removal in situ forming gel |
| url | https://www.mdpi.com/2310-2861/9/5/412 |
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