PMID- 36837696
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20230301
IS  - 2077-0375 (Print)
IS  - 2077-0375 (Electronic)
IS  - 2077-0375 (Linking)
VI  - 13
IP  - 2
DP  - 2023 Feb 3
TI  - Mannosylated-Chitosan-Coated Andrographolide Nanoliposomes for the Treatment of 
      Hepatitis: In Vitro and In Vivo Evaluations.
LID - 10.3390/membranes13020193 [doi]
LID - 193
AB  - A key diterpene lactone of Andrographis paniculata, i.e., andrographolide (AG), 
      exhibits a variety of physiological properties, including hepatoprotection. The 
      limited solubility, short half-life, and poor bioavailability limits the 
      pharmacotherapeutic potential of AG. Therefore, in this study we aimed to 
      formulate and optimize AG-loaded nanoliposomes (AGL) using the Design of 
      Experiment (DOE) approach and further modify the surface of the liposomes with 
      mannosylated chitosan to enhance its oral bioavailability. Physical, 
      morphological, and solid-state characterization was performed to confirm the 
      formation of AGL and Mannosylated chitosan-coated AGL (MCS-AGL). Molecular 
      docking studies were conducted to understand the ligand (MCS) protein (1EGG) type 
      of interaction. Further, in vitro release, ex vivo drug permeation, and in vivo 
      pharmacokinetics studies were conducted. The morphological studies confirmed that 
      AGL was spherical and a layer of MCS coating was observed on their surface, 
      forming the MCS-AGL. Further increase in the particle size and change in the zeta 
      potential of MCS-AGL confirms the coating on the surface of AGL (375.3 nm, 29.80 
      mV). The in vitro drug release data reflected a sustained drug release profile 
      from MCS-AGL in the phosphate buffer (pH 7.4) with 89.9 +/- 2.13% drug release in 8 
      h. Ex vivo permeation studies showed higher permeation of AG from MCS-AGL 
      (1.78-fold) compared to plain AG and AGL (1.37-fold), indicating improved 
      permeability profiles of MCS-AGL. In vivo pharmacokinetic studies inferred that 
      MCS-AGL had a 1.56-fold enhancement in AUC values compared to plain AG, 
      confirming that MCS-AGL improved the bioavailability of AG. Additionally, the 
      2.25-fold enhancement in the MRT proves that MCS coating also enhances the in 
      vivo stability and retention of AG (stealth effect). MCS as a polymer therefore 
      has a considerable potential for improving the intestinal permeability and 
      bioavailability of poorly soluble and permeable drugs or phytoconstituents when 
      coated over nanocarriers.
FAU - Metkar, Sayali Pravin
AU  - Metkar SP
AD  - Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal 
      Academy of Higher Education, Manipal 576104, Karnataka, India.
FAU - Fernandes, Gasper
AU  - Fernandes G
AUID- ORCID: 0000-0003-3625-2341
AD  - Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal 
      Academy of Higher Education, Manipal 576104, Karnataka, India.
FAU - Nikam, Ajinkya Nitin
AU  - Nikam AN
AUID- ORCID: 0000-0001-6268-6667
AD  - Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal 
      Academy of Higher Education, Manipal 576104, Karnataka, India.
FAU - Soman, Soji
AU  - Soman S
AD  - Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal 
      Academy of Higher Education, Manipal 576104, Karnataka, India.
FAU - Birangal, Sumit
AU  - Birangal S
AUID- ORCID: 0000-0001-7129-5748
AD  - Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical 
      Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka, India.
FAU - Seetharam, Raviraja N
AU  - Seetharam RN
AD  - Manipal Centre for Biotherapeutics Research, Manipal Academy of Higher Education, 
      Manipal 576104, Karnataka, India.
FAU - Joshi, Manjunath Bandu
AU  - Joshi MB
AD  - Department of Aging Research, Manipal School of Life Sciences, Manipal Academy of 
      Higher Education, Manipal 576104, Karnataka, India.
FAU - Mutalik, Srinivas
AU  - Mutalik S
AUID- ORCID: 0000-0002-0642-1928
AD  - Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal 
      Academy of Higher Education, Manipal 576104, Karnataka, India.
LA  - eng
GR  - GRD No.778/Vision Group of Science and Technology', Government of Karnataka 
      State, India/
PT  - Journal Article
DEP - 20230203
PL  - Switzerland
TA  - Membranes (Basel)
JT  - Membranes
JID - 101577807
PMC - PMC9965523
OTO - NOTNLM
OT  - andrographolide
OT  - bioavailability enhancement
OT  - liposomes
OT  - mannosylated chitosan
COIS- The authors declare no conflicts of interest.
EDAT- 2023/02/26 06:00
MHDA- 2023/02/26 06:01
PMCR- 2023/02/03
CRDT- 2023/02/25 03:36
PHST- 2022/12/16 00:00 [received]
PHST- 2023/02/01 00:00 [revised]
PHST- 2023/02/01 00:00 [accepted]
PHST- 2023/02/25 03:36 [entrez]
PHST- 2023/02/26 06:00 [pubmed]
PHST- 2023/02/26 06:01 [medline]
PHST- 2023/02/03 00:00 [pmc-release]
AID - membranes13020193 [pii]
AID - membranes-13-00193 [pii]
AID - 10.3390/membranes13020193 [doi]
PST - epublish
SO  - Membranes (Basel). 2023 Feb 3;13(2):193. doi: 10.3390/membranes13020193.