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Peer-reviewedCC BYFrontiers in Drug Delivery

Formulation and characterization of solid dispersion adsorbate of Candesartan Cilexetil: in vitro dissolution and in vivo performance

  • Harshad Makwana1
  • Anjali Patel1
  • Manisha Lalan2
  • Meenakshi Patel2
  • Nirmal Shah3
  • Bhavin Vyas1
  • Bhupendra Prajapati2
  • Pranav Shah4
4 affiliations
  1. 1Maliba Pharmacy College, Surat, India
  2. 2Parul University, Vadodara, India
  3. 3Sumandeep Vidyapeeth Deemed to be University, Vadodara, India
  4. 4Uka Tarsadia University, Surat, India
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Abstract

IntroductionCandesartan Cilexetil (CC) is a non-peptide angiotensin II type 1 receptor antagonist widely used in the treatment of hypertension. However, CC has poor aqueous solubility (0.006 ± 0.002 mg/mL), low oral bioavailability (15%) and undergoes significant first-pass metabolism.MethodsCandesartan Cilexetil Solid Dispersion adsorbate (CC-SDAs) was formulated by the fusion method, employing polyethylene glycol (PEG) 4000 as a hydrophilic carrier and Neusilin® US2 as an adsorbent, to improve the solubility, dissolution, and oral bioavailability of CC. The formulation was optimized using a 32 factorial design.Results and DiscussionThe optimized SDA formulation exhibited the following properties: Carr’s index (9.86 ± 0.09%), Hausner’s ratio (1.10 ± 0.16) and angle of repose (26.00 ± 0.19°), which shows improved flow property. DSC and XRD studies confirmed the conversion of the crystalline drug into an amorphous form. The optimized SDA formulation achieved %CDR of 90.41 ± 0.95% at Q30 min, demonstrating a marked improvement in in vitro dissolution compared to the pure drug (%CDR of 57.20 ± 3.78% at Q30 min). Furthermore, in vivo pharmacokinetic studies revealed a 2.02-fold enhanced oral bioavailability of CC from the SDA formulation compared to the CC suspension. Therefore, the SDA technique proves to be a promising approach for enhancing the solubility and dissolution of poorly water-soluble drugs.

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Cite

BibTeXRIS
BibTeX
@article{makwana2026formulation,
  title = {{Formulation and characterization of solid dispersion adsorbate of Candesartan Cilexetil: in vitro dissolution and in vivo performance}},
  author = {Harshad Makwana and Anjali Patel and Manisha Lalan and Meenakshi Patel and Nirmal Shah and Bhavin Vyas and Bhupendra Prajapati and Pranav Shah},
  journal = {Frontiers in Drug Delivery},
  year = {2026},
  month = oct,
  doi = {10.3389/fddev.2026.1975209},
  url = {https://doi.org/10.3389/fddev.2026.1975209},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - Formulation and characterization of solid dispersion adsorbate of Candesartan Cilexetil: in vitro dissolution and in vivo performance
AU  - Harshad Makwana
AU  - Anjali Patel
AU  - Manisha Lalan
AU  - Meenakshi Patel
AU  - Nirmal Shah
AU  - Bhavin Vyas
AU  - Bhupendra Prajapati
AU  - Pranav Shah
PY  - 2026
DA  - 2026/10/26
JO  - Frontiers in Drug Delivery
DO  - 10.3389/fddev.2026.1975209
UR  - https://doi.org/10.3389/fddev.2026.1975209
AB  - IntroductionCandesartan Cilexetil (CC) is a non-peptide angiotensin II type 1 receptor antagonist widely used in the treatment of hypertension. However, CC has poor aqueous solubility (0.006 ± 0.002 mg/mL), low oral bioavailability (15%) and undergoes significant first-pass metabolism.MethodsCandesartan Cilexetil Solid Dispersion adsorbate (CC-SDAs) was formulated by the fusion method, employing polyethylene glycol (PEG) 4000 as a hydrophilic carrier and Neusilin® US2 as an adsorbent, to improve the solubility, dissolution, and oral bioavailability of CC. The formulation was optimized using a 32 factorial design.Results and DiscussionThe optimized SDA formulation exhibited the following properties: Carr’s index (9.86 ± 0.09%), Hausner’s ratio (1.10 ± 0.16) and angle of repose (26.00 ± 0.19°), which shows improved flow property. DSC and XRD studies confirmed the conversion of the crystalline drug into an amorphous form. The optimized SDA formulation achieved %CDR of 90.41 ± 0.95% at Q30 min, demonstrating a marked improvement in in vitro dissolution compared to the pure drug (%CDR of 57.20 ± 3.78% at Q30 min). Furthermore, in vivo pharmacokinetic studies revealed a 2.02-fold enhanced oral bioavailability of CC from the SDA formulation compared to the CC suspension. Therefore, the SDA technique proves to be a promising approach for enhancing the solubility and dissolution of poorly water-soluble drugs.
SN  - 2674-0850
ER  -