Formulation, optimisation and evaluation of benidipine loaded lipid vesicles dissolving microneedles for transdermal delivery / (Record no. 102536)

MARC details
000 -LEADER
fixed length control field 04766ntm a2200337 i 4500
003 - CONTROL NUMBER IDENTIFIER
control field MY-KuUP
005 - DATE AND TIME OF LATEST TRANSACTION
control field 20251125111040.0
006 - FIXED-LENGTH DATA ELEMENTS--ADDITIONAL MATERIAL CHARACTERISTICS
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007 - PHYSICAL DESCRIPTION FIXED FIELD--GENERAL INFORMATION
fixed length control field ta
008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION
fixed length control field 250515t20242024my a|||fr|||| 000 0 eng d
020 ## - INTERNATIONAL STANDARD BOOK NUMBER
International Standard Book Number THE0010070 (Local)
Qualifying information Hardback
040 ## - CATALOGING SOURCE
Original cataloging agency UMPSA
Language of cataloging eng
Transcribing agency UMPSA
Description conventions rda
090 ## - LOCALLY ASSIGNED LC-TYPE CALL NUMBER (OCLC); LOCAL CALL NUMBER (RLIN)
Classification number (OCLC) (R) ; Classification number, CALL (RLIN) (NR) FTKKP .K43 2024 r Thesis
100 1# - MAIN ENTRY--PERSONAL NAME
Personal name Al-Japairai, Khater Ahmed Saeed,
Relator term author.
245 10 - TITLE STATEMENT
Title Formulation, optimisation and evaluation of benidipine loaded lipid vesicles dissolving microneedles for transdermal delivery /
Statement of responsibility, etc. Khater Ahmed Saeed Al-Japairai
264 #1 - PRODUCTION, PUBLICATION, DISTRIBUTION, MANUFACTURE, AND COPYRIGHT NOTICE
Place of production, publication, distribution, manufacture Kuantan Pahang :
Name of producer, publisher, distributor, manufacturer UMPSA
Date of production, publication, distribution, manufacture, or copyright notice 2024
264 #4 - PRODUCTION, PUBLICATION, DISTRIBUTION, MANUFACTURE, AND COPYRIGHT NOTICE
Date of production, publication, distribution, manufacture, or copyright notice © 2024
300 ## - PHYSICAL DESCRIPTION
Extent xi, 103 pages :
Other physical details illustrations ;
Dimensions 30 cm.+
Accompanying material 1 CD-ROM
336 ## - CONTENT TYPE
Source rdacontent
Content type term text
337 ## - MEDIA TYPE
Source rdamedia
Media type term unmediated
338 ## - CARRIER TYPE
Source rdacarrier
Carrier type term volume
347 ## - DIGITAL FILE CHARACTERISTICS
Source rda
File type text file
Encoding format PDF
500 ## - GENERAL NOTE
General note Faculty of Chemical and Process Engineering Technology
502 ## - DISSERTATION NOTE
Dissertation note Thesis (Doctor of Philosophy) -- Universiti Malaysia Pahang – 2024
504 ## - BIBLIOGRAPHY, ETC. NOTE
Bibliography, etc. note Includes bibliographical references
520 3# - SUMMARY, ETC.
Summary, etc. Benidipine (BEN) is a drug used for the treatment of hypertension. However, this drug suffers from extremely low oral bioavailability (only 20-30%) due to its poor aqueous solubility and extensive first-pass metabolism, thus limiting its efficacy for achieving optimal therapeutic levels. This study introduces a novel approach to address this significant drawback by developing BEN-loaded-lipid vesicles, namely transfersome, ethosome, and transethosome, which are then integrated into hyaluronic acid-based dissolving microneedles for transdermal application. In particular, the hypothesis proposes that this novel delivery system can effectively transport BEN through the skin by utilising the lipid vesicle’s ability to disrupt the stratum corneum and improve skin permeability, combined with hyaluronic acid-based dissolving microneedles that create microchannels, allowing for deeper skin penetration and ultimately leading to enhanced BEN bioavailability while bypassing the first-pass metabolism. In this study, the lipid vesicles were prepared using a thin-layer rotary evaporation method to produce unilamellar lipid vesicles and optimised by applying the Box-Behnken design. The results indicate that the optimised BEN-loaded transfersome (BEN-TF), ethosome (BEN-E), and transethosome (BEN-TE) showed vesicles sizes of 124.9 ± 1.49, 149.4 ± 3.81, and 168.3 ± 1.73 nm, with entrapment efficiencies (EE%) of 98.12 ± 0.18, 88.57 ± 0.38, and 96.42 ± 0.36%, and transdermal fluxes of 9.74 ± 0.53, 19.12 ± 0.19, and 20.21 ± 0.35 μg/cm2 /hr, respectively. It was found that DSC, ATR-FTIR, and XRD studies confirmed the amorphous state of BEN in the optimised formulations, while FESEM and HRTEM revealed a smooth, spherical morphology with nanosized, and uniform vesicular structures. CLSM clearly presented the depth of lipid vesicles’ permeation into the skin layers. The optimised lipid vesicles remained stable when stored at 4 °C for 3 months. Furthermore, the dissolving microneedles (DMNs) were prepared using 40% of hyaluronic acid and integrated with optimised BEN-TF, BEN-E, and BEN-TE formulations to provide further improvements in transdermal delivery. The resulting lipid-vesicles-loaded DMNs, including BEN-TF-DMNs, BEN-E-DMNs, and BEN-TEDMNs, exhibited sufficient mechanical strength, effective insertion into rat skin, and rapid dissolution. In the ex-vivo studies, the permeation coefficient of BEN was significantly improved using lipid-vesicle-loaded DMNs, compared with either optimised lipid vesicles alone or BEN-DMNs alone. In the in-vivo studies, the lipid vesicle-loaded DMNs improved the relative bioavailability of BEN by about 1.35, 1.58, and 1.86 times for BEN-TF-DMNs, BEN-E-DMNs, and BEN-TE-DMNs, respectively, compared to the oral-marketed BEN tablet. In comparison to BEN-DMNs, the relative bioavailability was enhanced by 2.49, 2.95, and 3.45 times for BEN-TF-DMNs, BEN-EDMNs, and BEN-TE-DMNs, respectively. This clearly indicates that BEN-TE-DMNs were superior to other lipid-vesicle-loaded DMNs. In conclusion, lipid vesicles combined with dissolving microneedles have shown high potential as carriers for transdermal delivery of benidipine. Further studies can be conducted to explore alternative polymers for DMN preparation, increase drug loading in the DMN arrays, validate formulations in diverse animal species, and evaluate patient satisfaction with the developed transdermal delivery system.
610 20 - SUBJECT ADDED ENTRY--CORPORATE NAME
Corporate name or jurisdiction name as entry element Faculty of Chemical and Process Engineering Technology
General subdivision Dissertations
650 #0 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element Universities and colleges
General subdivision Dissertations
650 #0 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element Theses
General subdivision Dissertations
942 ## - ADDED ENTRY ELEMENTS (KOHA)
Source of classification or shelving scheme Library of Congress Classification
Koha item type Thesis
Holdings
Withdrawn status Lost status Source of classification or shelving scheme Damaged status Not for loan Home library Current library Date acquired Total checkouts Full call number Barcode Date last seen Price effective from Koha item type
  Not lost Library of Congress Classification   Not for loan UMPLIB GAMBANG UMPLIB GAMBANG 15/05/2025   FTKKP .K43 2024 r Thesis T000003510 15/05/2025 15/05/2025 Thesis
  Not lost Library of Congress Classification     UMPLIB GAMBANG UMPLIB GAMBANG 15/05/2025   CD13739 T000003511 15/05/2025 15/05/2025 Thesis

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